ZK 216348

COA

级别和纯度:

≥98%

CAS编号: 669073-68-1
分子式: C₂₄H₂₃F₃N₂O₅
分子量: 476.45
PubChem编号: 9805004

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货号 (SKU)	包装规格	是否现货
Z651002-5mg	5mg	期货
Z651002-10mg	10mg	期货
Z651002-25mg	25mg	期货

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Immunology/Inflammation (1938) Vitamin D Related/Nuclear Receptor (908)

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基本描述

别名	售卖处
英文别名	(-)-ZK 216348 \| GTPL8643 \| HY-123352A \| (+)-Zk 216348 \| ZK 216348, (+)- \| 4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide \| E99033 \| (+)-4-(2,3-dihydrobenzofuran-7-yl)-2-hydro
规格或纯度	≥98%
英文名称	ZK 216348
生化机理	ZK 216348（(+)-ZK 216348）是一种非甾体类选择性糖皮质激素受体激动剂，IC 50 为 20.3 nM。ZK 216348 还能与黄体酮和矿质皮质激素受体结合，IC50 分别为 20.4 nM 和 79.9 nM。ZK 216348 还具有抗炎作用。
储存温度	2-8°C储存,避光,干燥
运输条件	冰袋运输
产品介绍	ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC 50 of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC 50 s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects In Vitro In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC 50 of 89 nM and 52 nM, respectively. Participation of an active GR in the antiinflammatory response of ZK 216348 is further investigated in Caco-2 cells, where the TNF-α-induced expression of the proinflammatory cytokine IL-8 is suppressed in the presence of ZK 216348. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo ZK 216348 (1-30 mg/kg; subcutaneous injection; for 24 hours; NMRI mice and Wistar rats) treatment inhibits ear edema in both mice and rats. A markedly superior side-effect profile is found in ZK 216348 with regard to increases in blood glucose, spleen involution, and, to a lesser extent, skin atrophy . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NMRI mice (26-28 g) and Wistar rats (140-160 g) injection with Croton oil Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg and 30 mg/kg Administration: Subcutaneous injection; for 24 hours Result: Inhibited ear edema in mice and rats. Form:Solid IC50& Target:IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor)
纯度	≥98%

关联靶点（人）

NR3C1 Tclin 糖皮质激素受体(Glucocorticoid receptor) (5 活性数据)

点击查看靶蛋白信息： NR3C1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

PGR Tclin 孕酮受体(Progesterone receptor) (2 活性数据)

点击查看靶蛋白信息： PGR

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

NR3C2 Tclin 盐皮质激素受体(Mineralocorticoid receptor) (2 活性数据)

点击查看靶蛋白信息： NR3C2

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)

点击查看靶蛋白信息： NR3C1

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

PGR Tclin Progesterone receptor (8562 活性数据)

点击查看靶蛋白信息： PGR

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

NR3C2 Tclin Mineralocorticoid receptor (2134 活性数据)

点击查看靶蛋白信息： NR3C2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

AR Tclin Androgen Receptor (11781 活性数据)

点击查看靶蛋白信息： AR

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

HFF (3142 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	小分子
IIUPAC Name	4-(2,3-dihydro-1-benzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamide
INCHI	1S/C24H23F3N2O5/c1-13-17-11-15(7-8-16(17)20(30)34-29-13)28-21(31)23(32,24(25,26)27)12-22(2,3)18-6-4-5-14-9-10-33-19(14)18/h4-8,11,32H,9-10,12H2,1-3H3,(H,28,31)
InChi Key	VRZVKIJRJRBQJT-UHFFFAOYSA-N
Smiles	CC1=NOC(=O)C2=C1C=C(C=C2)NC(=O)C(CC(C)(C)C3=CC=CC4=C3OCC4)(C(F)(F)F)O
Isomeric SMILES	CC1=NOC(=O)C2=C1C=C(C=C2)NC(=O)C(CC(C)(C)C3=CC=CC4=C3OCC4)(C(F)(F)F)O
关联CAS	669073-68-1
PubChem CID	9805004
MeSH Entry Terms	ZK 209614;ZK 216347;ZK 216348;ZK-209614;ZK-216347;ZK-216348;ZK209614;ZK216347;ZK216348
分子量	476.45

化学和物理性质

溶解性	DMSO : 200 mg/mL (419.77 mM; Need ultrasonic)
分子量	476.400 g/mol
XLogP3	4.300
氢键供体数Hydrogen Bond Donor Count	2
氢键受体数Hydrogen Bond Acceptor Count	9
可旋转键计数Rotatable Bond Count	5
精确质量Exact Mass	476.156 Da
单同位素质量Monoisotopic Mass	476.156 Da
拓扑极表面积Topological Polar Surface Area	97.200 Å²
重原子数Heavy Atom Count	34
形式电荷Formal Charge	0
复杂度Complexity	845.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	1
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

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