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Tanaproget,非甾体孕酮受体激动剂

规格或纯度: ≥99%
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Progesterone receptor Agonist
main product photo

基本描述

规格或纯度 ≥99%
英文名称 Tanaproget
生化机理

Description:
IC50 Value: 0.1 nM (EC50, induce alkaline phosphatase activity) [1]
Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins. Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives.
in vitro: In T47D cells, TNPR induces alkaline phosphatase activity with an EC(50) value of 0.1 nm, comparable with potent steroidal progestins such as medroxyprogesterone acetate (MPA) and trimegestone (TMG), albeit with a reduced efficacy ( approximately 60%). In a mammalian two-hybrid assay to measure PR agonist-induced interaction between steroid receptor co-activator-1 and PR, TNPR showed similar potency (EC(50) value of 0.02 nm) and efficacy to MPA and TMG [1].
in vivo: TNPR effectively down-regu

储存温度 -20°C储存
运输条件 超低温冰袋运输

名称和标识符

IUPAC Name 5-(4,4-dimethyl-2-sulfanylidene-1H-3,1-benzoxazin-6-yl)-1-methylpyrrole-2-carbonitrile
INCHI InChI=1S/C16H15N3OS/c1-16(2)12-8-10(4-6-13(12)18-15(21)20-16)14-7-5-11(9-17)19(14)3/h4-8H,1-3H3,(H,18,21)
InChi Key PYVFWTPEBMRKSR-UHFFFAOYSA-N
Canonical SMILES CC1(C2=C(C=CC(=C2)C3=CC=C(N3C)C#N)NC(=S)O1)C
分子式

C16H15N3OS
PubChem CID 4369524
分子量 297.37

化学和物理性质

溶解性 25°C: DMSO

安全信息

象形图
ghs08

Health Hazard

ghs07

Harmful
信号词 Danger
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H373: Causes damage to organs through prolonged or repeated exposure
H360: May damage fertility or the unborn child
预防措施声明 P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P260,P271,P304+P340,P403+P233,P362+P364,P203,P264+P265,P318,P337+P317,P332+P317,P319

靶标

Target ID 627
名称 Progesterone receptor
缩写名 SHP2
家族 3C. 3-Ketosteroid receptors
别名 CKR-L1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 933 11q22.1 PGR progesterone receptor
Mouse 2 926 9 A1 Pgr progesterone receptor
Rat 2 923 8q11 Pgr progesterone receptor
Entrez Gene 5241 (Hs) , 25154 (Rn) , 18667 (Mm)
OMIM 607311 (Hs)
UniProtKB P06401 (Hs) , Q63449 (Rn) , Q00175 (Mm)
RefSeq Nucleotide NM_000926 (Hs) , NM_022847 (Rn) , NM_008829 (Mm) , NM_001202474 (Hs)
RefSeq Protein NP_000917 (Hs) , NP_032855 (Mm) , NP_074038 (Rn) , NP_001189403 (Hs)
Ensembl Gene ENSG00000082175 (Hs) , ENSMUSG00000031870 (Mm) , ENSRNOG00000006831 (Rn)
Protein GI 112363098 (Mm) , 321117150 (Hs) , 12408292 (Rn)
NURSA Receptor 10.1621/9NIE3U3DI6 (Hs)
DrugBank Target P06401 (Hs)
CATH/Gene3D 3.30.50.10 (N/A)
ChEMBL Target CHEMBL208 (Hs) , CHEMBL2596 (Rn) , CHEMBL4969 (Mm)

关联配体

Ligand ID 7416
名称 tanaproget
别名 NSP-989
类别 Synthetic organic
学名 5-(4,4-dimethyl-2-sulfanylidene-2,4-dihydro-1H-3,1-benzoxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Tanaproget is an experimental nonsteroidal progesterone receptor agonist.

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