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3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037 |
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Product Name:A 987306;(±)-(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
Purity:99% HPLC Package:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
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| Company Name: |
EMMX Biotechnology LLC
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888-539-0666 |
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info@emmx.com |
| Products Intro: |
Product Name:A 987306
CAS:1082954-71-9
Purity:98% HPLC Package:5mg;10mg;25mg;50mg;100mg;250mg;500mg;1g
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| Company Name: |
MedBioPharmaceutical Technology Inc
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021-69568360 18916172912 |
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order@med-bio.cn |
| Products Intro: |
Product 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
Purity:98% Package:50mg; 10mg Remarks:Medbio
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| | (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine Basic information |
| Product Name: | (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine | | Synonyms: | (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine;A 987306;Benzofuro[2,3-h]quinazolin-2-amine, 5,6,7a,8,9,10,11,11a-octahydro-4-(1-piperazinyl)-, (7aR,11aR)-rel- | | CAS: | 1082954-71-9 | | MF: | C18H25N5O | | MW: | 327.42 | | EINECS: | | | Product Categories: | | | Mol File: | 1082954-71-9.mol | ![(±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine Structure](CAS/20180906/GIF/1082954-71-9.gif) |
| | (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine Chemical Properties |
| 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 |
| | (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine Usage And Synthesis |
| 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]. | | 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. |
| | (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine Preparation Products And Raw materials |
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