Vasopressin Receptor

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.

A64002

CAS No.

500170-27-4

d[Cha4]-AVP

d[Cha4]-AVP is a potent and selective agonist for the vasopressin V1b receptor, exhibiting a Ki value of 1.2 nM for the human V1b receptor. This compound demonstrates a marked selectivity for the V1b receptor over V1a, V2, and oxytocin receptors. d[Cha4]-AVP is useful in studies investigating the physiological and pathological roles of vasopressin signaling, particularly in neuroendocrine research and related therapeutic applications.

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.

A64004

CAS No.

192514-54-8

OPC-51803

OPC-51803 is an orally active nonpeptide agonist of the vasopressin V2 receptor. It demonstrates key biological activity in modulating water homeostasis and is particularly useful in the study of micturition disorders, including polyuria, nocturnal polyuria, and certain types of urinary incontinence. This compound serves as a valuable tool for investigating renal function and fluid regulation in various pathological conditions.

Cat. No.

A64005

CAS No.

2480-41-3

(Phe2,Orn8)-Oxytocin

(Phe2,Orn8)-Oxytocin is a selective agonist for the V1 vasopressin receptor. This compound is known to induce sustained contractility in rabbit epididymis tissues, with an EC50 value of 280 nM. Its potential applications include research in reproductive physiology and studies involving vasopressin receptor signaling pathways.

Cat. No.

A64006

CAS No.

1488411-60-4

Invopressin

Synonyms: OCE-205

Invopressin is a partial agonist of the V1A vasopressin receptor, exhibiting an EC50 of 1.0 nM. It is primarily utilized in research focused on cirrhosis-related conditions, including bacterial peritonitis, hepatorenal syndrome type 2 (HRS2), and refractory ascites. This compound enables the investigation of therapeutic strategies targeting vasopressin-mediated pathways in these clinical scenarios.

Cat. No.

A64008

CAS No.

1647120-04-4

Velmupressin acetate

Synonyms: c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2 acetate

Velmupressin acetate is a selective and potent agonist of the V2 receptor (V2R), exhibiting EC50 values of 0.07 nM and 0.02 nM for human and rat V2R, respectively. This peptidic compound is characterized by its short-acting nature, making it suitable for studies involving renal physiology and water homeostasis. Velmupressin acetate can be used in research applications focused on the modulation of water reabsorption and the investigation of vasopressin-related signaling pathways.

Cat. No.

A64009

CAS No.

2379889-71-9

Lazuvapagon

Synonyms: SK-1404; KRP-N118

Lazuvapagon is a selective agonist of the vasopressin V2 receptor, facilitating studies on water retention and renal function. This compound is primarily utilized in research to understand mechanisms underlying nocturia and other related renal pathologies. Its specificity for the V2 receptor makes it a valuable tool in pharmacological studies exploring vasopressin signaling and its effects on urinary output.

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.

A64011

CAS No.

914453-96-6

Terlipressin acetate

Terlipressin acetate is a selective agonist of the vasopressin V1 receptor, known for its strong vasoconstrictive effects. This compound effectively reduces splanchnic blood flow and portal pressure, making it useful in the management of acute variceal bleeding. Additionally, terlipressin exhibits anti-inflammatory and antioxidative properties, highlighting its potential in research related to hepatorenal syndrome and norepinephrine-resistant septic shock.

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.

A64015

CAS No.

1647119-71-8

c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm

c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm is a potent and selective agonist for the V2 vasopressin receptor (V2R), exhibiting effective activation with EC50 values of 0.25 nM for human V2R and 0.05 nM for rat V2R. This peptide compound has a short action profile, making it suitable for research applications focused on water homeostasis and kidney function. Its specificity for V2R positions it as a valuable tool in studying vasopressin signaling pathways and related physiological processes.

Cat. No.

A64016

CAS No.

1647119-61-6

Velmupressin

Synonyms: c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2

Velmupressin is a potent and selective peptidic agonist of the V2 receptor (V2R), with effective concentrations (EC50) of 0.07 nM for human V2R and 0.02 nM for rat V2R. This short-acting compound is utilized in research applications focusing on water conservation and aquaporin regulation, providing valuable insights into renal physiology and potential therapeutic interventions in conditions such as diabetes insipidus.

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.

A64019

CAS No.

16223-63-5

Khusimol

Khusimol is a vasopressin receptor ligand that plays a significant role in modulating cellular signaling pathways. It exhibits biological activities that may enhance the treatment of oral squamous cell carcinoma. This compound is primarily utilized in cancer research to explore its therapeutic potential and to better understand its mechanism of action in tumor biology.

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.

A64025

CAS No.

40944-53-4

[Asu1,6-Arg8]Vasopressin

[Asu1,6-Arg8]Vasopressin is a vasopressin agonist that activates the vasopressin receptor, leading to increased cyclic AMP accumulation and stimulating ACTH release in rat anterior pituitary cells in culture. This compound serves as a valuable tool in neuroendocrine research, particularly in studies involving the regulation of stress responses and hormonal activity. Its application may extend to investigations of pituitary function and vasopressin-mediated signaling 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.

Cat. No.

A64032

CAS No.

42061-33-6

D[LEU4,LYS8]-VP

D[LEU4,LYS8]-VP is a potent selective agonist of the vasopressin V1b receptor, demonstrating Ki values of 0.16 nM, 0.52 nM, and 1.38 nM for rat, human, and mouse V1b receptors, respectively. This compound exhibits distinct effects, including weak antidiuretic and vasopressor activities, as well as in vitro oxytocic properties. It is primarily utilized in research focused on the modulation of vasopressin-related pathways and studying the physiological roles of the V1b receptor in various biological systems.

Cat. No.

A64033

CAS No.

877856-17-2

VA-111913

Synonyms: VT-913

VA-111913 is a potent antagonist of the vasopressin receptor V1A, exhibiting a Ki value of 1.74 nM. This compound has demonstrated efficacy in reducing uterine contractions and enhancing uterine blood flow through the inhibition of vasopressin, making it relevant for studies focused on alleviating dysmenorrhea. VA-111913 serves as a valuable tool for research on menstrual pain and its associated mechanisms.

Cat. No.

A64034

CAS No.

1245620-47-6

Ribuvaptan

Ribuvaptan is a vasopressin receptor antagonist that plays a crucial role in cardiovascular research. This compound is primarily utilized for studying heart failure and related conditions. Through its mechanism of inhibiting vasopressin receptors, Ribuvaptan shows promise in elucidating the pathophysiology of heart failure and evaluating potential therapeutic strategies.