Vasopressin Receptor

Cat. No.

A11594

CAS No.

150683-30-0

Tolvaptan

Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM.

Cat. No.

A11638

CAS No.

168626-94-6

Conivaptan hydrochloride

Synonyms: YM 087

Conivaptan hydrochloride is a selective non-peptide antagonist of the vasopressin receptors, specifically targeting the V1A and V2 subtypes. With Ki values of 0.48 nM and 3.04 nM for the rat liver V1A receptor and rat kidney V2 receptor, respectively, it effectively inhibits vasopressin-mediated responses. This compound is primarily applied in research related to fluid balance disorders and the investigation of vasopressin receptor signaling pathways.

Cat. No.

A15784

CAS No.

131631-89-5

OPC21268

OPC21268 is a non-peptide AVP Receptor V (Vasopressin Receptor) antagonist that shows 1000-fold selectivity for V1 receptors over V2 receptors.

Cat. No.

A16188

CAS No.

909391-88-4

Vasopressin antagonist 1867

Synonyms: Compound 12i

Vasopressin antagonist, Orally available and selective V1b receptor antagonist (IC50 value 3 nM for hV1b inhibition, exhibiting >1000-fold selectivity over hV1a, hV2, and hOT).

Cat. No.

A16622

CAS No.

137975-06-5

Mozavaptan

Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM.

Cat. No.

A19373

CAS No.

1228088-30-9

Balovaptan

Synonyms: RG7314

Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.

Cat. No.

A21279

CAS No.

168079-32-1

Lixivaptan

Synonyms: VPA-985; WAY-VPA 985

Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.

Cat. No.

A21380

CAS No.

920022-47-5

RG7713

Synonyms: RO5028442

RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

Cat. No.

A22551

CAS No.

914453-95-5

Atosiban acetate

Synonyms: RW22164 acetate; RWJ22164 acetate

Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.

Cat. No.

A22924

CAS No.

77453-01-1

SKF 100398

Synonyms: d(CH2)5Tyr(Et)VAVP

SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.

Cat. No.

A23113

CAS No.

115150-59-9

Antagonist G

Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.

Cat. No.

A63995

CAS No.

150375-75-0

SR 49059

SR 49059 is a selective antagonist of the vasopressin V1a receptor, exhibiting a Ki value of 1.4 nM. This potent, orally active compound is utilized primarily in research to investigate the physiological and pathophysiological roles of vasopressin signaling. Its application includes studies related to cardiovascular function, water homeostasis, and stress responses.

Cat. No.

A63998

CAS No.

439687-69-1

Nelivaptan

Synonyms: SSR-149415

Nelivaptan is a selective, orally active antagonist of the vasopressin V1b receptor, exhibiting Ki values of 3.7 nM and 1.3 nM for native and recombinant rat V1b receptors, respectively. This compound effectively inhibits arginine vasopressin-induced calcium influx and secretion of corticotropin. Nelivaptan is valuable for research focused on stress, anxiety, and depression mechanisms.

Cat. No.

A64000

CAS No.

138470-70-9

Mozavaptan hydrochloride

Synonyms: OPC-31260 hydrochloride

Mozavaptan hydrochloride is a potent and selective antagonist of the vasopressin V2 receptor, exhibiting an IC50 of 14 nM. This benzazepine derivative demonstrates approximately 85-fold selectivity for the V2 receptor compared to the V1 receptor (IC50 of 1.2 μM) and effectively antagonizes the antidiuretic effects of arginine vasopressin (AVP) in vivo. It holds potential for research applications in treating conditions such as hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure.

Cat. No.

A64001

CAS No.

512784-93-9

SRX246

SRX246 is a highly selective antagonist of the vasopressin 1a (V1a) receptor, exhibiting a potent Ki of 0.3 nM for human V1a. It displays minimal interaction with V1b and V2 receptors, as well as negligible binding to 64 other receptor classes, including 35 G-protein-coupled receptors. This specificity enables SRX246 to be utilized in research focused on stress-related disorders and other conditions modulated by vasopressin activity.

Cat. No.

A64003

CAS No.

1642187-96-9

TASP0390325

TASP0390325 is a selective antagonist of the arginine vasopressin receptor 1B (V1B receptor), demonstrating high affinity and oral bioavailability. This compound exhibits significant antidepressant and anxiolytic effects, making it a valuable tool for research in mood disorders and anxiety-related conditions. Its mechanism of action facilitates the exploration of V1B receptor pathways in preclinical studies, assisting in the development of novel therapeutic strategies.

Cat. No.

A64010

CAS No.

1370444-22-6

Brezivaptan

Synonyms: Brezivaptanum; TH1773; TS-121

Brezivaptan is a selective vasopressin receptor antagonist that inhibits the activity of vasopressin, a key hormone involved in regulating water retention and blood pressure. This compound demonstrates potential therapeutic applications in conditions such as heart failure and hypertension by modulating renal and vascular function. Brezivaptan is an essential tool for research exploring the physiological roles of vasopressin and the development of related pharmacological interventions.

Cat. No.

A64012

CAS No.

942619-79-6

Tolvaptan phosphate ester sodium

Tolvaptan phosphate ester sodium is a prodrug that functions as a selective vasopressin receptor 2 (V2R) antagonist. It exhibits a competitive inhibition mechanism with an IC50 value of 1.28 μM against arginine vasopressin (AVP)-induced platelet aggregation. This compound is valuable for research into cardiac edema and related conditions, providing insights into the modulation of fluid balance and vascular function through vasopressin signaling pathways.

Cat. No.

A64013

CAS No.

129520-65-6

(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin

(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a selective antagonist of the vasopressin V1 receptor (VP V1R). This compound demonstrates a significant reduction in mean arterial pressure (MAP) in rat models, making it a valuable tool for studying cardiovascular regulation and the physiological roles of vasopressin. Its application in research may enhance understanding of hypertension and related disorders.

Cat. No.

A64017

CAS No.

2648650-50-2

Vasopressin V2 receptor antagonist 1

Vasopressin V2 receptor antagonist 1 functions as a selective antagonist of the vasopressin V2 receptor (V2R) with a Ki value of 3.8 nM. This compound is primarily utilized in research focusing on autosomal dominant polycystic kidney disease (ADPKD) and has potential implications in studying renal pathophysiology and therapeutics. Its specificity for V2R makes it a valuable tool for elucidating the receptor's role in kidney function and associated disorders.

Cat. No.

A64020

CAS No.

2145062-48-0

Enuvaptan

Synonyms: BAY-2327949

Enuvaptan is a selective vasopressin receptor antagonist that inhibits the actions of vasopressin at the V1 and V2 receptor sites. This compound demonstrates significant potential for research applications related to renal and cardiovascular diseases, particularly in understanding fluid balance and blood pressure regulation. Its ability to modulate vasopressin signaling makes it a valuable tool for investigating therapeutic strategies in conditions such as heart failure and hyponatremia.

Cat. No.

A64024

CAS No.

2355304-05-9

RGH-122

RGH-122 is a selective antagonist of the human V1a receptor, exhibiting high potency with a Ki value of 0.3 nM and an IC50 of 0.9 nM. This compound demonstrates favorable microsomal stability, with a clearance rate (CLint) of 13/28/25 μL/min/mg. RGH-122 is valuable for research applications involving vasopressin receptor signaling and related pathways.

Cat. No.

A64028

CAS No.

67269-08-3

Dp[Tyr(methyl)2,Arg8]-Vasopressin

Dp[Tyr(methyl)2,Arg8]-Vasopressin is a non-selective antagonist of the arginine vasopressin Vlb receptor. This compound is utilized primarily in studies investigating the regulation of water balance, blood pressure, and various physiological processes mediated by vasopressin receptors. Its application in research may extend to elucidating the receptor's role in cardiovascular and renal physiology.

Cat. No.

A64030

CAS No.

185913-78-4

Satavaptan

Synonyms: SR 121463

Satavaptan is a selective antagonist of the vasopressin V2 receptor. By inhibiting this receptor, Satavaptan modulates vasopressin-regulated phosphopeptides and disrupts vasopressin-mediated signaling pathways. This compound shows promise in the treatment of hyponatremia, making it a valuable tool for research in fluid balance and electrolyte homeostasis.

Cat. No.

A64031

CAS No.

745816-74-4

(D-Arg8)-Inotocin

(D-Arg8)-Inotocin is a highly selective and competitive antagonist of the vasopressin receptor subtype V1aR, exhibiting a Ki value of 1.3 nM. This compound demonstrates over 3000-fold selectivity for the human V1aR in comparison to other vasopressin receptor subtypes, including OTR, V1bR, and V2R. It is valuable for research applications focused on the modulation of V1aR-mediated pathways and can aid in studying its role in physiological and pathological processes.