(±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
![(±)-(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)
- CAS No.
- 1082954-71-9
- Chemical Name:
- (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
- 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-
- CBNumber:
- CB02518781
- Molecular Formula:
- C18H25N5O
- Molecular Weight:
- 327.42
- MDL Number:
- 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 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 |
| FDA UNII | 6BVK16R925 |
(±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine price More Price(7)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Tocris | 3640 | A987306 ≥98%(HPLC) | 1082954-71-9 | 10 | $261 | 2021-12-16 | Buy |
| Tocris | 3640 | A987306 ≥98%(HPLC) | 1082954-71-9 | 50 | $1046 | 2021-12-16 | Buy |
| Usbiological | 254492 | A 987306 | 1082954-71-9 | 10mg | $531 | 2021-12-16 | Buy |
| TRC | A965378 | A987306 | 1082954-71-9 | 2.5mg | $305 | 2021-12-16 | Buy |
| ApexBio Technology | B7451 | A987306 | 1082954-71-9 | 10mg | $402 | 2021-12-16 | Buy |
(±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
(±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| 3B Pharmachem (Wuhan) International Co.,Ltd. | 821-50328103-801 18930552037 | 3bsc@sina.com | China | 15848 | 69 |
| EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8449 | 60 |
| MedBioPharmaceutical Technology Inc | 021-69568360 18916172912 | order@med-bio.cn | China | 8141 | 58 |
| Changzhou Furuisi Biotechnology Co., Ltd | 0519-85524369 | 3477467573@qq.com | China | 8618 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24131 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4028 | 58 |
| ApexBio Technology | -- | sales@apexbt.com | United States | 6254 | 58 |