Carbonic-Anhydrase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Carbonic Anhydrase.html Carbonic HYPERLINK https:/www.MedChemE/Targets/Carbonic Anhydrase.html HYPERLINK https:/www.MedChemE/Targets/Carbonic Anhydrase.html AnhydraseCarbonate dehydrataseCarbonic anhydrase (CA) is a zinc-containing enzyme that catalyzes the rev

2、ersible hydration of carbon dioxide: CO + H O HCO - +2 2 3H+. Eight genetically distinct carbonic anhydrase enzyme families (-, -, - -, -, -, - and - CAs) were described to date.Carbonic anhydrases are involved in numerous physiological and pathological processes. Many of them are important therapeu

3、tictargets with the potential to be inhibited to treat a range of disorders including oedema, glaucoma, obesity, cancer, epilepsy, andosteoporosis.The carbonic anhydrase reaction is involved in many physiological and pathological processes, including respiration and transportof CO2 and bicarbonate b

4、etween metabolizing tissues and lungs; pH and CO2 homeostasis; electrolyte secretion in various tissuesand organs; biosynthetic reactions (such as gluconeogenesis, lipogenesis, and ureagenesis); bone resorption; calcification; andtumorigenicity. -CAs are Zn2+ metalloproteins expressed in animals, ve

5、rtebrates, prokaryotes, fungi, algae, protozoa, and plants.Sixteen mammalian -CA isoforms are known to be involved in many diseases such as glaucoma, edema, epilepsy, obesity, hypoxictumors, neuropathic pain, arthritis, neurodegeneration, etc.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Carb

6、onic Anhydrase.html Carbonic HYPERLINK https:/www.MedChemE/Targets/Carbonic Anhydrase.html HYPERLINK https:/www.MedChemE/Targets/Carbonic Anhydrase.html Anhydrase HYPERLINK https:/www.MedChemE/Targets/Carbonic Anhydrase.html HYPERLINK https:/www.MedChemE/Targets/Carbonic Anhydrase.html Inhibitors HY

7、PERLINK https:/www.MedChemE/e-dehydrodiconiferyl-alcohol.html (E)-Dehydrodiconiferyl HYPERLINK https:/www.MedChemE/e-dehydrodiconiferyl-alcohol.html HYPERLINK https:/www.MedChemE/e-dehydrodiconiferyl-alcohol.html alcoholCat. No.: HY-N2682A HYPERLINK https:/www.MedChemE/2-Aminobenzenesulfonamide.html

8、 2-Aminobenzenesulfonamide(Orthanilamide) Cat. No.: HY-B2147(E)-Dehydrodiconiferyl alcohol behaves as goodhCA IX and hCA XII dual inhibitors. And(E)-Dehydrodiconiferyl alcohol suppresses theNF-B nuclear translocation in connective tissueof healing area.2-Aminobenzenesulfonamide is a carbonic anhydra

9、se IXinhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/Acetazolamide.html Acetazolamide HYPERLINK https:/www.MedChemE/Acetazolamide.html HYPERLINK https:/www.Me

10、dChemE/acetazolamide-13c2-d3.html Acetazolamide-13C2,d3Cat. No.: HY-B0782 Cat. No.: HY-B0782S1Acetazolamide is a carbonic anhydrase (CA) IXinhibitor with an IC of 30 nM for .50 hCA IXDiuretic effects.Acetazolamide-13C2,d3 is the 13C- and deuteriumlabeled. Acetazolamide is a carbonic anhydrase(CA) IX

11、 inhibitor with an IC50 of 30 nM for hCAIX. Diuretic effects.Purity: 99.97%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 1 g, 5 gPurity: 98%Clinical Data:Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Acetazolamide-D3.html Acetazolamide-d3Cat. No.: HY-B0782S HYPERLINK https:/www.MedChemE/benzolam

12、ide.html Benzolamide(CL11366) Cat. No.: HY-118467Acetazolamide D3 is deuterium labeledAcetazolamide, which is a potent carbonicanhydrase (CA) inhibitor.Benzolamide (CL11366) is a potent carbonicanhydrase (CA) inhibitor, with Ks of 15 nM, 9inM, 94 nM and 78 nM for hCA I, hCA II, EcoCA andVchCA, respe

13、ctively. Benzolamide also inhibitsCAS3, with a K of 54 nM. Benzolamide can be usedifor the research of glaucoma and seizures.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98.07%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLI

14、NK https:/www.MedChemE/Benzthiazide.html Benzthiazide HYPERLINK https:/www.MedChemE/Benzthiazide.html HYPERLINK https:/www.MedChemE/benzthiazide-d7.html Benzthiazide-d7Cat. No.: HY-B1424 Cat. No.: HY-B1424SBenzthiazide is a long-acting diuretic and ahypertension agent. Benzthiazide is an inhibitorof

15、 carbonic anhydrase 9 (CA9), with Ks of 8.0,i8.8 and 10 nM for CA9, CA2 and CA1, respectively.Benzthiazide also suppresses proliferation ofcancer cells.Benzthiazide-d7 is the deuterium labeledBenzthiazide. Benzthiazide is a long-actingdiuretic and a hypertension agent. Benzthiazide isan inhibitor of

16、 carbonic anhydrase 9 (CA9), withKs of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1,irespectively.Purity: 99.40%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 2.5 mg, 25 mg HYPERLINK https:/www.MedChemE/Brinzolamide.html Brinzo

17、lamide HYPERLINK https:/www.MedChemE/Brinzolamide.html HYPERLINK https:/www.MedChemE/brinzolamide-d5.html Brinzolamide-d5(AL-4862) Cat. No.: HY-B0588 (AL-4862-d5) Cat. No.: HY-B0588SBrinzolamide(AL 4862) is a potent carbonicanhydrase II inhibitor with IC50 of 3.19 nM.Brinzolamide-d5 (AL-4862-d5) is

18、the deuteriumlabeled Brinzolamide. Brinzolamide (AL 4862) is apotent carbonic anhydrase II inhibitor with IC of503.19 nM.Purity: 99.33%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 E

19、mail: salesMedChemE HYPERLINK https:/www.MedChemE/caix-inhibitor-s4.html CAIX HYPERLINK https:/www.MedChemE/caix-inhibitor-s4.html HYPERLINK https:/www.MedChemE/caix-inhibitor-s4.html Inhibitor HYPERLINK https:/www.MedChemE/caix-inhibitor-s4.html HYPERLINK https:/www.MedChemE/caix-inhibitor-s4.html

20、S4 HYPERLINK https:/www.MedChemE/caix-inhibitor-s4.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-10.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-10.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-10.html anhydrase HYPERLINK https:/www.Med

21、ChemE/carbonic-anhydrase-inhibitor-10.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-10.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-10.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-10.html 10Cat. No.: HY-110243 Cat. No.: HY-115994CAIX

22、Inhibitor S4 is a potent and selectiveinhibitor of carbonic anhydrase IX/XII (CA IX/XII),with a K of 7 nM and 2 nM, respectively. CAIXiInhibitor S4 also inhibits CA II and CA I (K=546iand 5600 nM, respectively).Carbonic anhydrase inhibitor 10 is a potent hCA IXinhibitor with a K value of 6.2 nM. Car

23、bonicianhydrase inhibitor 10 exhibits anti-proliferativeactivity against MCF-7 cancer cell line with anIC of 11.9 M. Carbonic anhydrase inhibitor 1050can be used for cancer research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize

24、: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html

25、HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html 11 HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-11.html HYPERLINK https:/ww

26、w.MedChemE/carbonic-anhydrase-inhibitor-12.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-12.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-12.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-12.html HYPERLINK https:/www.MedChemE/ca

27、rbonic-anhydrase-inhibitor-12.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-12.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-12.html 12Cat. No.: HY-115998 Cat. No.: HY-115999Carbonic anhydrase inhibitor 11 (compound VI) is apotent, selective carbonic anh

28、ydrase inhibitor.Carbonic anhydrase inhibitor 11 shows K values ofi40, 39, 200 and 900 nM against CA II, IX, and XII,respectively.Carbonic anhydrase inhibitor 12 is a potent CA IIinhibitor, also has inhibitory activity in CA I(Ks of 1.72 and 271 nM in CA II and CA I,irespectively). Carbonic anhydras

29、e inhibitor 12 haspotent anticancer activity against differentcancer cell lines.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-2.html Carbonic HYPERLINK http

30、s:/www.MedChemE/carbonic-anhydrase-inhibitor-2.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-2.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-2.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/

31、carbonic-anhydrase-inhibitor-2.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-2.html 2 HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-2.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-3.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibi

32、tor-3.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-3.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-3.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-3.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-3.html HYPER

33、LINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-3.html 3Cat. No.: HY-142849 Cat. No.: HY-142853Carbonic anhydrase inhibitor 3 (compound 7c) is acarbonic anhydrase II inhibitor. Carbonic anhydraseinhibitor 3 reduces the intraocular pressure inglaucomatous rabbits.Carbonic anhydrase inhibitor 3

34、(compound 11g) is acarbonic anhydrase II inhibitor. Carbonic anhydraseinhibitor 3 reduces the intraocular pressure inglaucomatous rabbits.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/c

35、arbonic-anhydrase-inhibitor-4.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-4.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-4.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-4.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase

36、-inhibitor-4.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-4.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-4.html 4 HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-4.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-5.html Carbon

37、ic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-5.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-5.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-5.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-5.html inhibitor HYPERLINK htt

38、ps:/www.MedChemE/carbonic-anhydrase-inhibitor-5.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-5.html 5Cat. No.: HY-144376 Cat. No.: HY-144639Carbonic anhydrase inhibitor 4 is carbonicanhydrase photoprobe/inhibitor. Carbonicanhydrase inhibitor 4 is against human carbonicanhydrases (

39、hCA I-XIV) with K values of 640-1166inM.Carbonic anhydrase inhibitor 5 is a potent andselective human carbonic anhydrase (hCA)inhibitor with IC s of 42.9, 47,6 and 6.7 nM for50hCA II, hCA IX and hCA XII, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinica

40、l Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-6.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-6.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-6.html anhydrase HYPERLINK https:/www.MedChemE/carbo

41、nic-anhydrase-inhibitor-6.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-6.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-6.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-6.html 6 HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-

42、6.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-7.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-7.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-7.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-7.html HYPERLINK

43、https:/www.MedChemE/carbonic-anhydrase-inhibitor-7.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-7.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-7.html 7Cat. No.: HY-144640 Cat. No.: HY-144641Carbonic anhydrase inhibitor 6 (compound 9b) is apotent inhibi

44、tor of human carbonic anhydrase(hCA), with Ks of 9.7 nM, 35.2 nM, 88.5 nM, andi91.8 nM for hCA IX, hCA II, hCA XII and hCA I,respectively.Carbonic anhydrase inhibitor 7 (compound 5b) is apotent inhibitor of human carbonic anhydrase(hCA), with Ks of 6.5 nM, 7.1 nM, 72.1 nM, andi255.8 nM for hCA IX, h

45、CA II, hCA XII and hCA I,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-8.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anh

46、ydrase-inhibitor-8.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-8.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-8.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-8.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor

47、-8.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-8.html 8 HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-8.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-9.html Carbonic HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-9.html HYPERLINK https:/

48、www.MedChemE/carbonic-anhydrase-inhibitor-9.html anhydrase HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-9.html HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-9.html inhibitor HYPERLINK https:/www.MedChemE/carbonic-anhydrase-inhibitor-9.html HYPERLINK https:/www.MedChemE/car

49、bonic-anhydrase-inhibitor-9.html 9Cat. No.: HY-115984 Cat. No.: HY-144807Carbonic anhydrase inhibitor 8 (compound R-13), abenzyl-derivative, is a potent human carbonicanhydrase (hCA) inhibitor with K values of 60.7inM, 320.7 nM, 2298 nM for hCA I, hCA II, hCA IV,respectively.Carbonic anhydrase inhib

50、itor 9 is a potent carbonicanhydrase (CA) inhibitor with Ks of 56.4 andi56.9nM for hCA II and IX, respectively.Antiproliferative activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/c

51、lofenamide.html Clofenamide(Aquedux) Cat. No.: HY-119919 HYPERLINK https:/www.MedChemE/Dichlorphenamide.html Dichlorphenamide(Diclofenamide) Cat. No.: HY-B0397Clofenamide (Aquedux) is a carbonic anhydrase (CA)inhibitor. Clofenamide exhibits diuretic activity.Dichlorphenamide(Diclofenamide) is a carb

52、onicanhydrase inhibitor that is used in the treatmentof glaucoma.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.39%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Dimethylfraxetin.html Dimethylfraxetin(6,7,8-Trimethoxycoumarin;

53、 Fraxetin dimethyl ether) Cat. No.: HY-N0085 HYPERLINK https:/www.MedChemE/Dorzolamide.html Dorzolamide(L671152; MK507) Cat. No.: HY-B0109Dimethylfraxetin is a Carbonic anhydraseinhibitor, with a K value of 0.0097 M.iDorzolamide (L671152) is a potent carbonicanhydrase II inhibitor, with IC values of

54、 0.1850nM and 600 nM for red blood cell CA-II and CA-Irespectively. Dorzolamide possesses anti-tumoractivity.Purity: 99.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Dorzolamide-hydrochlor

55、ide.html Dorzolamide HYPERLINK https:/www.MedChemE/Dorzolamide-hydrochloride.html HYPERLINK https:/www.MedChemE/Dorzolamide-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Dorzolamide-hydrochloride.html HYPERLINK https:/www.MedChemE/dorzolamide-d5.html Dorzolamide-d5(L671152 hydrochlo

56、ride; MK507 hydrochloride) Cat. No.: HY-B0109ACat. No.: HY-B0109SDorzolamide (L671152) hydrochloride is a potentcarbonic anhydrase II inhibitor, with IC values50of 0.18 nM and 600 nM for red blood cell CA-II andCA-I respectively. Dorzolamide possessesanti-tumor activity.Dorzolamide-d5 (L671152-d5) i

57、s the deuteriumlabeled Dorzolamide. Dorzolamide (L671152) is apotent carbonic anhydrase II inhibitor, with IC50values of 0.18 nM and 600 nM for red blood cellCA-II and CA-I respectively. Dorzolamide possessesanti-tumor activity.Purity: 99.91%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100

58、 mgPurity: 98%Clinical Data:Size: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/emac10101d.html EMAC10101d HYPERLINK https:/www.MedChemE/emac10101d.html HYPERLINK https:/www.MedChemE/Ethoxzolamide.html EthoxzolamideCat. No.: HY-138365(Redupresin; L-643786; PNU-4191) Cat. No.: HY-B1480EMAC10101d is a pot

59、ent and selective toward hCA IIinhibitor, with a K of 8.1 nM.iEthoxzolamide is a carbonic anhydrase inhibitorwith K of 1 nM.iPurity: 99.89%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.43%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg4 Tel: 609-228-6898 Fax

60、: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/fluorometholone-acetate.html Fluorometholone HYPERLINK https:/www.MedChemE/fluorometholone-acetate.html HYPERLINK https:/www.MedChemE/fluorometholone-acetate.html acetateCat. No.: HY-B1471 HYPERLINK https:/www.MedChemE/girentuximab.ht