| Identification | Back Directory | [Name]
(±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine | [CAS]
1082954-71-9 | [Synonyms]
A 987306
(±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
Benzofuro[2,3-h]quinazolin-2-amine, 5,6,7a,8,9,10,11,11a-octahydro-4-(1-piperazinyl)-, (7aR,11aR)-rel- | [Molecular Formula]
C18H25N5O | [MOL File]
1082954-71-9.mol | [Molecular Weight]
327.42 |
| Chemical Properties | Back Directory | [Boiling point ]
630.7±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
<32.74mg/ml in DMSO; <32.74mg/ml in ethanol | [form ]
solid | [pka]
8.70±0.10(Predicted) | [color ]
Off-white |
| Hazard Information | Back Directory | [Uses]
A 987306 is an H4 receptor antagonist and has been studied as an H4 modulator towards the potential treatment of diseases. | [Biological Activity]
a987306,cis-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quin- azolin-2-amine[1], is a selective and potent h4 receptor antagonist [2].h4r is one of 4 known g-protein-coupled receptors (h1, h2, h3 and h4 receptors) of histamine. it is for mediating some physiological functions of histamine [3].in a cell-based ca2+-flux functional assay, a 987306 had no activation to the receptor, but blocked the h4r activation induced by endogenous histamine. a 987306 potently decreased histamine-mediated binding between rat h4-receptor-containing membranes and gtp-γ-[35s] with a kb of 6 nm [3].in sprague-dawley rats, after ip injection, a 987306 had a favorable fractional bioavailability (fip/iv =72%), a half-life of 4.7 h and a cmax of 1.73 μm at a tmax of 0.25 h after dosing. after oral dosing, a 987306 had a moderate fractional oral bioavailability (fpo/iv =26%) with a half-life of 3.7 h and a cmax of 0.30 μm at a tmax of 1.5 h after dosing. the plasma protein binding of a 987306 measured in rats was found to be 59% [3].to human h4r and rat h4r, the ki values of a 987306 are 5.8 nm and 3.4 nm, respectively. a 987306 reduced scratch responses in mice with an ed50 of 0.36 μmol/kg. a 987306 was found to be selective and bear an ic50 > 810 nm for over 100 kinases [3]. | [in vivo]
A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) is found to reduce scratching induced by the histamine H4 agonist clobenpropit (HY-101198)[1].
A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (Fpo/iv=26%) with a half-life of 3.7 h and a Cmax of 0.30 μM at a Tmax of 1.5 h after dosing[1].
| Animal Model: | Mice[1] | | Dosage: | 98.23 μg/kg , 327.42 μg/kg, 982.26 μg/kg, 9.82 mg/kg (Pharmacokinetic Analysis) | | Administration: | Intraperitoneal injection | | Result: | Fpo/iv=26%, T1/2=3.7 hours, Cmax=0.30 μM, Tmax=1.5 hours |
| [storage]
Store at -20°C | [References]
[1]. vanina a. medina and elena s. rivera. histamine receptors and cancer pharmacology. british journal of pharmacology, 2010, 161:755-767.
[2]. m.i. strakhova, c.a. cuff, a.m. manelli, et al. in vitro and in vivo characterization of a-940894: a potent histamine h4 receptor antagonist with anti-inflammatory properties. british journal of pharmacology, 2009, 157:44-54.
[3]. huaqing liu, robert j. altenbach, tracy l. carr, et al. cis-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (a-987306), a new histamine h4r antagonist that blocks pain responses against carrageenan-induced hyperalgesia. j. med. chem., 2008, 51:7094-7098. |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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