福尔霉素A

福尔霉素A用途

Formycin A (NSC 102811) 是一种嘌呤核苷抗生素,一种有效的人类免疫缺陷病毒 1 型 (HIV-1) 的抑制剂,EC50 为 10 μM。Formycin A 显示抗肿瘤和抗病毒活性。
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福尔霉素A名称

[ CAS 号 ]:
6742-12-7

[ 中文名 ]:
间型霉素A

[ 英文名 ]:
formycin A

[英文别名 ]:

福尔霉素A生物活性

[ 描述 ]:

Formycin A (NSC 102811) 是一种嘌呤核苷抗生素,一种有效的人类免疫缺陷病毒 1 型 (HIV-1) 的抑制剂,EC50 为 10 μM。Formycin A 显示抗肿瘤和抗病毒活性。

[ 相关类别 ]:

研究领域 >> 癌症
信号通路 >> 抗感染 >> HIV
研究领域 >> 感染

[ 靶点 ]

HIV-1:10 μM (EC50)


[体外研究]

福尔马霉素A(NSC 102811;1μM,5μM,10μM)拮抗齐多夫定(AZT;双脱氧核苷链终止剂)。

[参考文献]

[1]. Dapp MJ , et al. Discovery of novel ribonucleoside analogs with activity against human immunodeficiency virus type 1.J Virol. 2014 Jan;88(1):354-63.

[2]. Zhang M, et al. Comparative Investigation into Formycin A and Pyrazofurin A Biosynthesis Reveals Branch Pathways for the Construction of C-Nucleoside Scaffolds. Appl Environ Microbiol. 2020 Jan 7;86(2).

福尔霉素A物理化学性质

[ 密度 ]:
1.771g/cm3

[ 沸点 ]:
709.5ºC at 760 mmHg

[ 熔点 ]:
153-155ºC

[ 分子式 ]:
C10H13N5O4

[ 分子量 ]:
285.25700

[ 闪点 ]:
382.9ºC

[ 精确质量 ]:
285.10700

[ PSA ]:
159.63000

[ 折射率 ]:
1.803

[ 储存条件 ]:
-20°C

福尔霉素AMSDS

福尔霉素A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UR0719000
CHEMICAL NAME :
1H-Pyrazolo(4,3-d)pyrimidine, 7-amino-3-beta-D-ribofuranosyl-
CAS REGISTRY NUMBER :
6742-12-7
LAST UPDATED :
199612
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C10-H13-N5-O4
MOLECULAR WEIGHT :
267.28
WISWESSER LINE NOTATION :
T56 BMN FN HNJ IZ D- BT5OTJ CQ DQ E1Q

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 :
1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
400 mg/kg
TOXIC EFFECTS :
Blood - hemorrhage Blood - changes in spleen Blood - other changes
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
125 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
250 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
20 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
165 mg/kg/5D-I
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Parenteral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
200 mg/kg/8D-I
TOXIC EFFECTS :
Related to Chronic Data - death

MUTATION DATA

TYPE OF TEST :
Mutation test systems - not otherwise specified
TEST SYSTEM :
Rodent - mouse Leukocyte
DOSE/DURATION :
25700 ug/L
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 30,481,1987
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福尔霉素A安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 安全声明 (欧洲) ]:
22-24/25

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

[ RTECS号 ]:
UR0719000

福尔霉素A文献

Purine nucleoside metabolism in the erythrocytes of patients with adenosine deaminase deficiency and severe combined immunodeficiency.

J. Clin. Invest. 57(4) , 1025-35, (1976)

Deficiency of erythrocytic and lymphocytic adenosine deaminase (ADA) occurs in some patients with severe combined immunodeficiency disease (SCID). SCID with ADA deficiency is inherited as an autosomal...

The riddle of formycin A insulinotropic action.

Biochem. Mol. Med. 57(1) , 47-63, (1996)

Formycin A augments insulin release evoked by glucose (5.6 mm or more), this effect not being rapidly reversible. The mechanism responsible for the insulinotropic action of formycin A was investigated...

Tautomerism of the nucleoside antibiotic formycin, as studied by carbon-13 nuclear magnetic resonance.

J. Am. Chem. Soc. 95(14) , 4761-2, (1973)


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