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阿帕泛

阿帕泛用途

Apafant (WEB 2086) 是一种有效的血小板活化因子 (PAF) 拮抗剂,抑制 PAF 结合人 PAF 受体的 Ki 值为 9.9 nM。

阿帕泛名称

[ CAS 号 ]:
105219-56-5

[ 中文名 ]:
阿帕泛

[ 英文名 ]:
Apafant

[中文别名 ]:

阿帕芬特

[英文别名 ]:

Apafant

阿帕泛生物活性

[ 描述 ]:

Apafant (WEB 2086) 是一种有效的血小板活化因子 (PAF) 拮抗剂,抑制 PAF 结合人 PAF 受体的 Ki 值为 9.9 nM。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[ 靶点 ]

Ki: 9.9 nM (Platelet-activating factor)[1]

[参考文献]

[1]. Kato M, et al. Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs. J Pharmacol Sci. 2004 Aug;95(4):435-42.

阿帕泛物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
720.2±70.0 °C at 760 mmHg

[ 熔点 ]:
186-188ºC

[ 分子式 ]:
C₂₂H₂₂ClN₅O₂S

[ 分子量 ]:
455.96

[ 闪点 ]:
389.4±35.7 °C

[ 精确质量 ]:
455.118286

[ PSA ]:
100.85000

[ LogP ]:
1.32

[ 外观性状 ]:
白色至灰色粉末

[ 蒸汽压 ]:
0.0±2.3 mmHg at 25°C

[ 折射率 ]:
1.734

[ 储存条件 ]:
2-8°C

阿帕泛MSDS

详细MSDS(安全技术说明书)

阿帕泛毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QE0479700

CHEMICAL NAME :: Morpholine, 4-((4-(2-chlorophenyl)-9-methyl-6H-thieno(3,2-f)(1,2, 4)triazolo(4,3-a)(1,4) diazepin-2-yl)-1-oxopropyl)-

CAS REGISTRY NUMBER :: 105219-56-5

LAST UPDATED :: 199706

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C22-H22-Cl-N5-O2-S

MOLECULAR WEIGHT :: 456.00

WISWESSER LINE NOTATION :: T B575 AN CS HN KNN GHJ D2V- AT6N DOTJ& GR BG M1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4968794

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4968794 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 36 gm/kg

SEX/DURATION :: female 6-12 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 52,215,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3250 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Fertility - abortion Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 52,209,1996

阿帕泛安全信息

[ 危害码 (欧洲) ]:
Xn

[ 危险品运输编码 ]:
NONH for all modes of transport

阿帕泛文献

A pepducin derived from the third intracellular loop of FPR2 is a partial agonist for direct activation of this receptor in neutrophils but a full agonist for cross-talk triggered reactivation of FPR2.

PLoS ONE 9(10) , e109516, (2014)

We recently described a novel receptor cross-talk mechanism in neutrophils, unique in that the signals generated by the PAF receptor (PAFR) and the ATP receptor (P2Y2R) transfer formyl peptide recepto...

Neutrophils reduce the parasite burden in Leishmania (Leishmania) amazonensis-infected macrophages.

PLoS ONE 5(11) , e13815, (2010)

Studies on the role of neutrophils in Leishmania infection were mainly performed with L. (L) major, whereas less information is available for L. (L) amazonensis. Previous results from our laboratory s...

Effect of sodium tanshinone IIA sulfonate treatment in a rat model of preeclampsia.

Am. J. Physiol. Regul. Integr. Comp. Physiol. 308(3) , R163-72, (2015)

Preeclampsia is a disorder of pregnancy with a significant impact on maternal and fetal health. The complexity of this multifactorial condition has precluded development of effective therapies and, al...

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阿帕泛