A histamine H4 receptor agonist (Ki = 31.6 nM); selective for histamine H4 over H1 and H3 receptors in radioligand binding assays (Kis = >1 and 1 µM

VUF8430 (hydrobromide) – 1 mg

Brand:
Cayman
CAS:
100130-32-3
Storage:
-20
UN-No:
Non-Hazardous - /

VUF8430 is a histamine H4 receptor agonist (Ki = 31.6 nM).{53487} It is selective for histamine H4 over H1 and H3 receptors in radioligand binding assays (Kis = >1 and 1 µM, respectively) and is less active in isolated guinea pig atria, which endogenously expresses high levels of H2 receptors (pD2 = 3.8). VUF8430 inhibits forskolin-induced, cAMP-mediated increases in β-galactosidase activity (EC50 = 50.1 nM). In vivo, VUF8430 (30 mg/kg) enhances HCl-induced formation of gastric lesions in rats.{51085} It also reduces mechanical and thermal allodynia in a mouse model of peripheral neuropathy induced by spared nerve injury (SNI).{53488}  

 

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SKU: 27682 - 1 mg Category:

Description

A histamine H4 receptor agonist (Ki = 31.6 nM); selective for histamine H4 over H1 and H3 receptors in radioligand binding assays (Kis = >1 and 1 µM, respectively) and is less active in isolated guinea pig atria, which endogenously expresses high levels of H2 receptors (pD2 = 3.8); inhibits forskolin-induced, cAMP-mediated increases in β-galactosidase activity (EC50 = 50.1 nM); enhances HCl-induced formation of gastric lesions in rats at 30 mg/kg; reduces mechanical and thermal allodynia in a mouse model of SNI-induced peripheral neuropathy

Formal name: carbamimidothioic acid, 2-[(aminoiminomethyl)amino]ethyl ester, dihydrobromide

Synonyms: 

Molecular weight: 323.1

CAS: 100130-32-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Immunology & Inflammation|Gastric Disease|Peptic Ulcers||Research Area|Neuroscience|Pain Research

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