CI-949
目录号 : GC31994
CI-949是一种过敏介质释放抑制剂，可抑制组胺(histamine)，白三烯C4/D4(LTC4/LTD4)和血栓素B2(TXB2)的释放，IC50分别为11.4μM，0.5μM和0.1μM。
Cas No.:104961-19-5
Sample solution is provided at 25 µL, 10mM.
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CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.
CI-949 inhibits, in a dose-dependent manner, the release of histamine, leukotriene, and thromboxane from human basophilic leukocytes challenged with anti-IgE. The IC50 for inhibition of histamine release is 11.4 μM. Virtually complete inhibition of histamine release occurs at 100 μM, with negligible inhibition of release <3 μM. Both LTC4/LTD4 and TXB2 release are inhibited at lower concentrations (IC50, 0.5 and 0.1 μM, respectively). Complete inhibition of leukotriene and thromboxane synthesis/release is obtained with 10 and 1 μM of CI-949, respectively. CI-949 is an effective inhibitor of release of all three mediators in response to this stimulus. The IC50s for inhibition of histamine, leukotriene, and thromboxane are 6.3, 2, and 0.1 μM for FMLP challenge[1]. CI-949 effectively inhibits the release of histamine and the synthesis or release of immunoreactive sulfidopeptide leukotrienes C4-D4 and thromboxane B2 from antigen-challenged lung fragments of of actively sensitized guinea-pigs. The IC50s are 26.7±2.8 μM for histamine, 2.7±2.4 μM for leukotriene, and 3.0±1.8 μM for thromboxane[2].
Actively sensitized guinea-pigs are given i .p. doses of 30, 50, or 100 mg/kg of CI-949 between 20-120 min before aerosol challenge with antigen. A dose of 50 mg/kg i.p. of CI-949 protects conscious, aerosol-allergen challenged guinea-pigs for at least 1 h and 100 mg/kg i.p. or per os protects for at least 2 h. The animals are protected from collapse for at least I h after 50 and 100 mg/kg, and 100 mg/kg afforded complete protection up to 2h. An oral dose of 100 mg/kg at 2 h, but not at 4 h before challenge also inhibits collapse. A dose of 100 mg/kg at 4 h and again at 2 h before challenge is more effective than a single dose at 2 h[2].
[1]. Conroy MC, et al. Inhibition of histamine, leukotriene C4/D4, and thromboxane B2 release from human leukocytes and human chopped lung mast cells by the allergic mediator release inhibitor, CI-949. J Allergy Clin Immunol. 1990 Dec;86(6 Pt 1):902-8. [2]. Adolphson RL, et al. CI-949: a new, potential antiallergy compound inhibits antigen-induced allergic reactions in guinea-pigs in vitro and in vivo. Pulm Pharmacol. 1990;3(4):203-8.
Kinase experiment: | Inhibition by Cl-949 of LTC4/D4, TXB2, and histamine release from human leukoeytes challenged with anti-lgE. Cells are preincubated at 37°C with Cl-949 (0.1, 1, 10 and 100 μM) for 10 minutes before the addition of anti-lgE. The cells are then challenged with appropriate stimulus in a concentration to obtain histamine release from the ascending portion of the dose-response curve from each donor (or with buffer) and incubated for 50 minutes at 37°C. The reaction is stopped by centrifugation, and the resulting supernatant solutions are decanted and saved for quantitation of allergic mediators. Mediator release and inhibition of mediator release by CI-949 is comparable in ceils prepared by either method[1]. |
Animal experiment: | Guinea pigs[2]Male, Hartley Strain guinea-pigs, weighing 175-250 g are used in these experiments. Actively sensitized guinea-pigs are given i.p. doses of 30, 50, or 100 mg/kg of CI-949 between 20-120 min before aerosol challenge with antigen[2]. |
References: [1]. Conroy MC, et al. Inhibition of histamine, leukotriene C4/D4, and thromboxane B2 release from human leukocytes and human chopped lung mast cells by the allergic mediator release inhibitor, CI-949. J Allergy Clin Immunol. 1990 Dec;86(6 Pt 1):902-8. | |
| Cas No. | 104961-19-5 | SDF | |
| Canonical SMILES | O=C(C(N1C2=CC=CC=C2)=C(OC(C)C)C3=C1C=CC(OC)=C3)NC4=NN=NN4 | ||
| 分子式 | C20H20N6O3 | 分子量 | 392.41 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5484 mL | 12.7418 mL | 25.4836 mL |
| 5 mM | 0.5097 mL | 2.5484 mL | 5.0967 mL |
| 10 mM | 0.2548 mL | 1.2742 mL | 2.5484 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00%
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