A 987306 |
| Catalog No.GC17743 |
A 987306 es un potente antagonista de histamina H4 biodisponible por vía oral, con Kis de 3,4 nM y 5,8 nM para H4 de rata y H4 humano.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1082954-71-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1082954-71-9 | SDF | |
| Chemical Name | (7aR,11aR)-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine | ||
| Canonical SMILES | NC(N=C1N2CCNCC2)=NC3=C1CCC4=C3[C@@H](CCCC5)[C@@H]5O4 | ||
| Formula | C18H25N5O | M.Wt | 327.42 |
| Solubility | <32.74mg/ml in DMSO; <32.74mg/ml in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0542 mL | 15.2709 mL | 30.5418 mL |
| 5 mM | 610.8 μL | 3.0542 mL | 6.1084 mL |
| 10 mM | 305.4 μL | 1.5271 mL | 3.0542 mL |
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Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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