Vasopressin-Receptor-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html Vasopressin HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html ReceptorThe neurohypophysial hormone arginine vasopressin (AVP) is involved in diverse function

2、s including regulation of body fluidhomeostasis, vasoconstriction, and adrenocorticotropic hormone release. These physiological effects are mediated by three subtypes of vasopressin receptors, designated V , V (or V ), and V . They all belong to the large rhodopsin-like G-protein-coupled1a 1b 3 2rec

3、eptor family.The V receptor is expressed in both neuronal and non-neuronal tissues including the heart and elicits a variety of physiological1aeffects including cell contraction and proliferation, stimulation of hepatic glycogenolysis, platelet aggregation and coagulation factor release. The V recep

4、tor subtype is found predominantly in the pituitary gland where it stimulates adrenocorticotropic1bhormone release. Both the V and V AVP receptors act through a G protein alpha-subunit of the G family (q, q11, q14,1a 1b q15/16) to activate phospholipase C-, and, thus enhance cellular IP3 and calcium

5、 levels. By contrast, the V receptor subtype is2localized predominantly to the kidney where it mediates the anti-diuretic effects of AVP through the heterotrimeric G protein Gsand activation of adenylyl cyclase.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html Vasopressi

6、n HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html Agonists HYPERLINK https:/www.Med

7、ChemE/Targets/Vasopressin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html HYPERLINK https:/www.MedChemE/Targets/Vasopressin Receptor.html Antagonists HYPERLINK https:/www.MedChemE/antagonist-g.html Antago

8、nist HYPERLINK https:/www.MedChemE/antagonist-g.html HYPERLINK https:/www.MedChemE/antagonist-g.html G HYPERLINK https:/www.MedChemE/antagonist-g.html HYPERLINK https:/www.MedChemE/antagonist-g-tfa.html Antagonist HYPERLINK https:/www.MedChemE/antagonist-g-tfa.html HYPERLINK https:/www.MedChemE/anta

9、gonist-g-tfa.html G HYPERLINK https:/www.MedChemE/antagonist-g-tfa.html HYPERLINK https:/www.MedChemE/antagonist-g-tfa.html TFACat. No.: HY-P1185 Cat. No.: HY-P1185AAntagonist G is a potent vasopressin antagonist.Antagonist G is also a weak antagonist of GRP andBradykinin. Antagonist G induces AP-1t

10、ranscription and sensitizes cells tochemotherapy.Antagonist G TFA is a potent vasopressinantagonist. Antagonist G is also a weak antagonistof GRP and Bradykinin. Antagonist G induces AP-1transcription and sensitizes cells tochemotherapy.Purity: 95.0%Clinical Data: No Development ReportedSize: 1 mg,

11、5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Argipressin.html Argipressin(Arg8-vasopressin; AVP) Cat. No.: HY-P0049 HYPERLINK https:/www.MedChemE/Atosiban.html Atosiban(RW22164; RWJ22164) Cat. No.: HY-17572Argipressin (Arg8-vasopressin) binds to

12、 the V1,V2, V3-vascular arginine vasopressin receptor,with a K value of 1.31 nM in A7r5 rat aorticdsmooth muscle cells for V1.Atosiban (RW22164; RWJ22164) is a nonapeptidecompetitive vasopressin/oxytocin receptorantagonist, and is a desamino-oxytocin analogue.Atosiban is the main tocolytic agent and

13、 has thepotential for spontaneous preterm labor research.Purity: 99.82%Clinical Data: LaunchedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.09%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/atosiban-acetate.html Atosiban HYPERLINK https:/www.M

14、edChemE/atosiban-acetate.html HYPERLINK https:/www.MedChemE/atosiban-acetate.html acetate(RW22164 acetate; RWJ22164 acetate) Cat. No.: HY-17572A HYPERLINK https:/www.MedChemE/Balovaptan.html Balovaptan(RG7314) Cat. No.: HY-109024Atosiban acetate (RW22164 acetate;RWJ22164acetate) is a nonapeptide com

15、petitivevasopressin/oxytocin receptor antagonist, and is adesamino-oxytocin analogue. Atosiban is the maintocolytic agent and has the potential forspontaneous preterm labor research.Balovaptan (RG7314) is an orally available,selective brain-penetrant vasopressin 1a (hV1a)receptor antagonist, with Ks

16、 of 1 and 39 nM forihuman (hV1a) and mouse (mV1a) receptors, and isused for the research of autism.Purity: 99.92%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.18%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/big-endoth

17、elin-1-1-38-human.html Big HYPERLINK https:/www.MedChemE/big-endothelin-1-1-38-human.html HYPERLINK https:/www.MedChemE/big-endothelin-1-1-38-human.html Endothelin-1 HYPERLINK https:/www.MedChemE/big-endothelin-1-1-38-human.html HYPERLINK https:/www.MedChemE/big-endothelin-1-1-38-human.html (1-38),

18、HYPERLINK https:/www.MedChemE/big-endothelin-1-1-38-human.html HYPERLINK https:/www.MedChemE/big-endothelin-1-1-38-human.html human HYPERLINK https:/www.MedChemE/big-endothelin-1-1-38-human.html HYPERLINK https:/www.MedChemE/big-endothelin-1-1-39-porcine.html Big HYPERLINK https:/www.MedChemE/big-en

19、dothelin-1-1-39-porcine.html HYPERLINK https:/www.MedChemE/big-endothelin-1-1-39-porcine.html Endothelin-1 HYPERLINK https:/www.MedChemE/big-endothelin-1-1-39-porcine.html HYPERLINK https:/www.MedChemE/big-endothelin-1-1-39-porcine.html (1-39), HYPERLINK https:/www.MedChemE/big-endothelin-1-1-39-por

20、cine.html HYPERLINK https:/www.MedChemE/big-endothelin-1-1-39-porcine.html porcineCat. No.: HY-P2538 Cat. No.: HY-P2539Big Endothelin-1 (1-38), human is the precursor ofendothelin-1. Endothelin-1 (ET-1) is a potentvasopressor peptide.Big Endothelin-1 (1-39), porcine is the precursorof endothelin-1.

21、Endothelin-1 (ET-1) is a potentvasopressor peptide. Big Endothelin-1 (1-39),porcine has similar pressor effects in vivo.Purity: 98%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Conivaptan-hydrochloride.

22、html Conivaptan HYPERLINK https:/www.MedChemE/Conivaptan-hydrochloride.html HYPERLINK https:/www.MedChemE/Conivaptan-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Conivaptan-hydrochloride.html HYPERLINK https:/www.MedChemE/d-cha4-avp.html dCha4-AVP(YM 087) Cat. No.: HY-18347ACat. No

23、.: HY-P1390Conivaptan (hydrochloride) is a non-peptideantagonist of vasopressin receptor, with K valuesiof 0.48 and 3.04 nM for rat liver V1A receptor andrat kidney V2 receptor respectively.dCha4-AVP is a potent and selective vasopressin(AVP) V1b receptor agonist with a K of 1.2 nMifor human V1b rec

24、eptor. dCha4-AVP shows moreselective for V1b receptor than human V1areceptor, V2 receptor, and oxytocin receptors.Purity: 99.92%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 99.27%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg2 Tel: 609-228-6898 Fax: 609-228-590

25、9 Email: salesMedChemE HYPERLINK https:/www.MedChemE/d-cha4-avp-tfa.html dCha4-AVP HYPERLINK https:/www.MedChemE/d-cha4-avp-tfa.html HYPERLINK https:/www.MedChemE/d-cha4-avp-tfa.html TFA HYPERLINK https:/www.MedChemE/d-cha4-avp-tfa.html HYPERLINK https:/www.MedChemE/d-leu4-lys8-vp.html DLEU4,LYS8-VP

26、Cat. No.: HY-P1390A Cat. No.: HY-P1163dCha4-AVP TFA is a potent and selectivevasopressin (AVP) V1b receptor agonist with a Kof 1.2 nM for human V1b receptor. dCha4-AVPTFA shows more selective for V1b receptor thanhuman V1a receptor, V2 receptor, and oxytocinreceptors.iDLEU4,LYS8-VP is a selective ag

27、onist ofvasopressin V receptor1b , with the Kis of 0.16nM, 0.52 nM, and 0.1.38 nM for rat, human andmouse V receptor, respectively.1bDLEU4,LYS8-VP has weak antidiuretic,vasopressor, and in vitro oxytocic activities.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical

28、Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/d-leu4-lys8-vp-tfa.html DLEU4,LYS8-VP HYPERLINK https:/www.MedChemE/d-leu4-lys8-vp-tfa.html HYPERLINK https:/www.MedChemE/d-leu4-lys8-vp-tfa.html TFACat. No.: HY-P1163A HYPERLINK https:/www.MedChemE/enuvaptan.html Enuvaptan(

29、BAY-2327949) Cat. No.: HY-139572DLEU4,LYS8-VP TFA is a selective agonist ofvasopressin V1b receptor Kis, with the of 0.16nM, 0.52 nM, and 0.1.38 nM for rat, human andmouse V receptor, respectively.1bDLEU4,LYS8-VP TFA has weak antidiuretic,vasopressor, and in vitro oxytocic activities.Enuvaptan (BAY-

30、2327949) is a vasopressin receptorantagonist and has the potential for research intorenal and cardiovascular diseases.Purity: 98.16%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fedovapagon.html

31、FedovapagonCat. No.: HY-14887 HYPERLINK https:/www.MedChemE/Felypressin.html Felypressin(PLV-2) Cat. No.: HY-A0182Fedovapagon is a selective vasopressin V2 receptor(V2R) agonist with an EC of 24 nM, which is50being developed for the treatment of nocturia.Felypressin (PLV-2) is a non-catecholaminevas

32、oconstrictor and a vasopressin 1 agonist.Felypressin is widely used in dental procedures.Purity: 99.14%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.68%Clinical Data: LaunchedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/felypressin-acetate.h

33、tml Felypressin HYPERLINK https:/www.MedChemE/felypressin-acetate.html HYPERLINK https:/www.MedChemE/felypressin-acetate.html acetate HYPERLINK https:/www.MedChemE/felypressin-acetate.html HYPERLINK https:/www.MedChemE/OPC-21268.html Fuscoside(PLV-2 acetate) Cat. No.: HY-A0182A (OPC-21268) Cat. No.:

34、 HY-15009Felypressin acetate (PLV-2 acetate) is anon-catecholamine vasoconstrictor and a vasopressin1 agonist. Felypressin acetate is widely used indental procedures.Fuscoside (OPC-21268) is an orally effective,nonpeptide, vasopressin V1 receptor antagonistwith an IC of 0.4 M.50Purity: 98%Clinical D

35、ata: Phase 4Size: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/l-371-257.html L-371,257 HYPERLINK https:/www.MedChemE/l-371-257.html HYPERLINK https:/www.MedChemE/lazuvapagon.html LazuvapagonCat. No.: H

36、Y-15010(SK-1404; KRP-N118) Cat. No.: HY-109181L-371,257 is an orally bioavailable,non-blood-brain barrier penetrant, selective andcompetitive antagonist of oxytocin receptor(pA2=8.4) with high affinity at both the oxytocinreceptor (K=19 nM) andi vasopressin V1a receptor(K=3.7 nM).iPurity: 98.83%Clin

37、ical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgLazuvapagon (SK-1404) is a vasopressin V2 receptoragonist for the research of nocturia.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Lixivaptan.html Lixivaptan(VPA

38、-985; WAY-VPA 985) Cat. No.: HY-14185 HYPERLINK https:/www.MedChemE/Mozavaptan.html Mozavaptan(OPC-31260) Cat. No.: HY-18346Lixivaptan (VPA-985, WAY-VPA 985) is an orallyactive and selective vasopressin receptor V2antagonist, with IC values of 1.2 and 2.3 nM for50human and rat V2, respectively.Mozav

39、aptan (OPC-31260) is a benzazepine derivativeand a potent, selective, competitive and orallyactive vasopressin V receptor antagonist with an2IC of 14 nM.50Purity: 99.90%Clinical Data: Phase 3Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.89%Clinical Data: LaunchedSize: 10 mM 1 m

40、L, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/mozavaptan-hydrochloride.html Mozavaptan HYPERLINK https:/www.MedChemE/mozavaptan-hydrochloride.html HYPERLINK https:/www.MedChemE/mozavaptan-hydrochloride.html hydrochloride(OPC-31260 hydrochloride) Cat. No.: HY-123593 HYPERLINK https:/www.MedCh

41、emE/mozavaptan-d6.html Mozavaptan-d6(OPC-31260-d6) Cat. No.: HY-18346SMozavaptan hydrochloride (OPC-31260 hydrochloride)is a benzazepine derivative and a potent,selective, competitive and orally activevasopressin V2 receptor antagonist with an IC50of 14 nM.Mozavaptan-d6 (OPC-31260-d6) is the deuteri

42、umlabeled Mozavaptan. Mozavaptan (OPC-31260) is abenzazepine derivative and a potent, selective,competitive and orally active vasopressin V2receptor antagonist with an IC of 14 nM.50Purity: 98.16%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development Re

43、portedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/RO5028442.html RG7713(RO5028442) Cat. No.: HY-12981 HYPERLINK https:/www.MedChemE/skf-100398.html SKF HYPERLINK https:/www.MedChemE/skf-100398.html HYPERLINK https:/www.MedChemE/skf-100398.html 100398(d(CH2)5Tyr(Et)VAVP) Cat. No.: HY-P3066RG7713 (

44、RO5028442) is a highly potent andselective Brain-Penetrant Vasopressin 1a (V1a)receptor antagonist with Kis of 1 nM (hV1a) and39 nM (mV1a).SKF 100398 (d(CH2)5Tyr(Et)VAVP), an argininevasopressin (AVP) analogue, is a specificantagonist of the antidiuretic effect of exogenousand endogenous AVP.Purity:

45、 99.79%Clinical Data: Phase 1Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/SR_49059.html SR HYPERLINK https:/www.MedChemE/SR_49059.html HYPERLINK https:/www.MedChemE/SR_49059.html 49059 HYPERLINK ht

46、tps:/www.MedChemE/SR_49059.html HYPERLINK https:/www.MedChemE/srx-246.html SRX246Cat. No.: HY-18345 Cat. No.: HY-105685SR 49059 (SR-49059) is a potent, orally active,selective vasopressin V1a antagonist with a Kivaule of 1.4 nM.SRX246 is a potent, CNS-penetrant, highlyselective, orally bioavailable

47、vasopressin 1a (V1a)receptor antagonist (K=0.3 nM for human V1a).iSRX246 has no interaction at V1b and V2 receptors.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.69%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.M

48、edChemE/tasp0390325.html TASP0390325 HYPERLINK https:/www.MedChemE/tasp0390325.html HYPERLINK https:/www.MedChemE/Terlipressin.html TerlipressinCat. No.: HY-117820 Cat. No.: HY-12554TASP0390325 is a high affinity and orally activearginine vasopressin receptor 1B (V1B receptor)antagonist with antidep

49、ressant and anxiolyticactivities.Terlipressin is a vasopressin analogue with potentvasoactive properties. Terlipressin is a highlyselective vasopressin V1 receptor agonist thatreduces the splanchnic blood flow and portalpressure and controls acute variceal bleeding.Purity: 98%Clinical Data: No Devel

50、opment ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/terlipressin-acetate.html Terlipressin HYPERLINK https:/www.MedChemE/terlipressin-acetate.html HYPERLINK https:/ww

51、w.MedChemE/terlipressin-acetate.html acetate HYPERLINK https:/www.MedChemE/terlipressin-acetate.html HYPERLINK https:/www.MedChemE/terlipressin-d5.html Terlipressin-d5Cat. No.: HY-12554A Cat. No.: HY-12554STerlipressin acetate is a vasopressin analoguewith potent vasoactive properties. Terlipressina

52、cetate is a highly selective vasopressin V1receptor agonist that reduces the splanchnicblood flow and portal pressure and controls acutevariceal bleeding.Terlipressin-d5 is the deuterium labeledTerlipressin. Terlipressin is a vasopressinanalogue with potent vasoactive properties.Purity: 99.76%Clinic

53、al Data: LaunchedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Tolvaptan.html Tolvaptan(OPC-41061) Cat. No.: HY-17000 HYPERLINK https:/www.MedChemE/tolvaptan-d7.html Tolvaptan-D7Cat. No.: HY-17000STolvaptan is a selective, competitive argini