| Identification | Back Directory | [Name]
2-(diaminomethylideneamino)ethylsulfanylmethanimidamide dihydrobromide | [CAS]
100130-32-3 | [Synonyms]
VUF8430 hydrobromide VUF 8430 dihydrobromide >=97% (NMR) 2-guanidinoethyl carbamimidothioate dihydrobromide 2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester 2-(diaminomethylideneamino)ethylsulfanylmethanimidamide dihydrobromide | [Molecular Formula]
C4H13Br2N5S | [MDL Number]
MFCD01694605 | [MOL File]
100130-32-3.mol |
| Chemical Properties | Back Directory | [storage temp. ]
room temp | [solubility ]
deionized water: soluble24mg/mL | [form ]
solid | [color ]
White to off-white | [Water Solubility ]
deionized water: 24mg/mL |
| Hazard Information | Back Directory | [Description]
VUF8430 is a histamine H4 receptor agonist (Ki = 31.6 nM). 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. It also reduces mechanical and thermal allodynia in a mouse model of peripheral neuropathy induced by spared nerve injury (SNI). | [Uses]
VUF 8430 Dihydrobromide is an H4 receptor agonist. | [IC 50]
H4 receptor | [storage]
Desiccate at RT | [References]
[1] HERMAN D. LIM. Discovery of S-(2-Guanidylethyl)-isothiourea (VUF 8430) as a Potent Nonimidazole Histamine H4 Receptor Agonist[J]. Journal of Medicinal Chemistry, 2006, 49 23: 6650-6651. DOI: 10.1021/jm060880d [2] GABRIELLA CORUZZI . Selective histamine H3 and H4 receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach[J]. European journal of pharmacology, 2011, 669 1: Pages 121-127. DOI: 10.1016/j.ejphar.2011.07.038 [3] MARIA DOMENICA SANNA. Histamine H4 receptor agonist-induced relief from painful peripheral neuropathy is mediated by inhibition of spinal neuroinflammation and oxidative stress[J]. British Journal of Pharmacology, 2016, 174 1: 28-40. DOI: 10.1111/bph.13644 |
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BOC Sciences
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Energy Chemical
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