產(chǎn)品目錄

規(guī)格	5mg 10mg 25mg 100mg
CAS	732983-37-8
別名	BAY61-3606
化學(xué)名	2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide
分子式	C20H18N6O3
分子量	390.4
溶解度	<4.01mg/mL in EtOH, <3.9mg/mL in H2O
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

The spleen tyrosine kinase plays important roles in various inflammation pathways through affecting both the FcεRI-mediated signaling in mast cells and basophils and the FcγR-mediated signaling in macrophages and neutrophils. Therefor syk is thought to be an attractive target for the treatment of related respiratory diseases such as asthma and allergy. As a potent and selective inhibitor of syk, BAY 61-3606 dose-dependently inhibited syk activity with IC50 value of 10 nM and competed against ATP with Ki value of 7.5 nM. It showed no significant effects on other tyrosine kinases including Src, Fyn, Lyn, Btk and Itk at concentration up to 4.7 μM. BAY 61-3606 inhibited the inflammation-related cell functions in various inflammatory cells. It also showed potent anti-allergic and anti-asthmatic activities in animal models [1].

In the ratbasophilic leukemia cell line, RBL-2H3 cells, treatment of BAY 61-3606 inhibited the FcεRI-mediated hexosaminidase release with IC50 value of 46 nM. In rat peritoneal mast cells, BAY 61-3606 inhibited FcεRI-mediated Serotonin release with IC50 value of 17 nM. In HCMC cells, BAY 61-3606 inhibited the release of tryptase and histamine with IC50 values of 5.5 and 5.1 nM, respectively. BAY 61-3606 also suppressed BCR-induced increases of intracellular calcium concentration with IC50 value of 81 nM. Besides that, BAY 61-3606 was reported to inhibit the FcγR-mediated superoxide production in U937 cells with IC50 value of 52 nM [1].

In rats with type-I allergic reactions, oral administration of BAY 61-3606inhibited the PCA reaction dose-dependently with ED50 value of 8 mg/kg. In an asthmatic model, administration of BAY 61-3606 at dose of 3 mg/kg significantly inhibited the increase of pulmonary pressure stimulated by DNP-BSA. In addition, administration of BAY 61-3606 at dose of 30 mg/kg resulted in the inhibition of eosinophil accumulation in BAL fluid [1].

References:

[1] Yamamoto N, Takeshita K, Shichijo M, Kokubo T, Sato M, Nakashima K, Ishimori M, Nagai H, Li YF, Yura T, Bacon KB. The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther. 2003 Sep;306(3):1174-81.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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