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甲基泼尼松龙

规格或纯度: 98%

CAS编号: 83-43-2
分子式: C₂₂H₃₀O₅
分子量: 374.47
Beilstein号: 2340300
EC号: 201-476-4
MDL号: MFCD00010591
PubChem编号: 6741

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货号 (SKU)	包装规格	是否现货
M420133-250mg	250mg	现货
M420133-1g	1g	现货
M420133-5g	5g	现货
M420133-25g	25g	现货

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Glucocorticoid receptor Agonist TRPC5 Activator

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基本描述

规格或纯度	98%
英文名称	6-α-Methylprednisolone
别名	甲泼尼龙；甲基强的松龙
英文别名	U 7532；Methylprednisolone；(6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
生化机理	Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
储存温度	2-8°C储存,避光
运输条件	冰袋运输
产品介绍	Methylprednisolone 是皮质类固醇，可作用于糖皮质激素受体。Methylprednisolone 通过激活 ACE2 并降低 IL-6 水平来改善严重的 COVID-19。

名称和标识符

EC号	201-476-4
IUPAC Name	(6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
INCHI	InChI=1S/C22H30O5/c1-12-8-14-15-5-7-22(27,18(26)11-23)21(15,3)10-17(25)19(14)20(2)6-4-13(24)9-16(12)20/h4,6,9,12,14-15,17,19,23,25,27H,5,7-8,10-11H2,1-3H3/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1
InChi Key	VHRSUDSXCMQTMA-PJHHCJLFSA-N
Canonical SMILES	CC1CC2C3CCC(C3(CC(C2C4(C1=CC(=O)C=C4)C)O)C)(C(=O)CO)O
分子式	C₂₂H₃₀O₅
PubChem CID	6741
Beilstein号	2340300
分子量	374.47

数据库链接

DrugBank Ligand	DB00959
PubChem CID	6741
CAS Registry No.	83-43-2
ChEMBL Ligand	CHEMBL650
Wikipedia	Methylprednisolone
ChEBI	CHEBI:6888
NURSA Ligand	10.1621/6A7WO8R4WE
PEP	methylprednisolone
Immunopaedia Search	methylprednisolone
DrugCentral Ligand	1768

化学和物理性质

溶解性	insoluble in H2O; ≥15.35 mg/mL in DMSO; ≥9.5 mg/mL in EtOH with ultrasonic
敏感性	对光敏感
熔点	237°C(lit.)

安全信息

象形图	Health Hazard Harmful
信号词	Danger
危险声明	H373: Causes damage to organs through prolonged or repeated exposure H302: Harmful if swallowed H312: Harmful in contact with skin H372: Causes damage to organs through prolonged or repeated exposure H360: May damage fertility or the unborn child H361: Suspected of damaging fertility or the unborn child
预防措施声明	P280,P302+P352,P321,P405,P501,P264,P260,P270,P362+P364,P330,P203,P301+P317,P318,P317,P319
WGK Germany	2
RTECS	TU4146000
Reaxy-Rn	2340300
个人防护装备	Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter

靶标

Target ID

490

名称

TRPC5

缩写名

SHP2

家族

Transient Receptor Potential channels (TRP)

别名

MIP-1αRL-2 (mouse)

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	6	973	Xq23	TRPC5	transient receptor potential cation channel subfamily C member 5
Rat	6	974	Xq14	Trpc5	transient receptor potential cation channel, subfamily C, member 5
Mouse	6	975	X 65.49 cM	Trpc5	transient receptor potential cation channel, subfamily C, member 5

OMIM

300334 (Hs)

Entrez Gene

140933 (Rn) , 22067 (Mm) , 7224 (Hs)

UniProtKB

Q9QX29 (Mm) , Q9UL62 (Hs)

RefSeq Protein

NP_036603 (Hs) , NP_543174 (Rn) , NP_033454 (Mm)

RefSeq Nucleotide

NM_012471 (Hs) , NM_080898 (Rn) , NM_009428 (Mm)

Ensembl Gene

ENSG00000072315 (Hs) , ENSMUSG00000041710 (Mm) , ENSRNOG00000027233 (Rn)

Protein GI

18266704 (Rn) , 6912736 (Hs) , 6678435 (Mm)

CATH/Gene3D

1.25.40.20 (N/A)

ChEMBL Target

CHEMBL4523481 (Mm) , CHEMBL1250411 (Hs)

Target ID

625

名称

Glucocorticoid 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	777	5q31.3	NR3C1	nuclear receptor subfamily 3 group C member 1
Mouse	2	783	18 21.09 cM	Nr3c1	nuclear receptor subfamily 3, group C, member 1
Rat	2	795	18p11	Nr3c1	nuclear receptor subfamily 3, group C, member 1

Entrez Gene

2908 (Hs) , 24413 (Rn) , 14815 (Mm)

OMIM

138040 (Hs)

UniProtKB

P04150 (Hs) , P06536 (Rn) , P06537 (Mm)

RefSeq Nucleotide

NM_000176 (Hs) , NM_012576 (Rn) , NM_008173 (Mm)

RefSeq Protein

NP_000167 (Hs) , NP_032199 (Mm) , NP_036708 (Rn) , NP_001018661 (Hs) , NP_001019265 (Hs) , NP_001191194 (Hs)

Ensembl Gene

ENSG00000113580 (Hs) , ENSMUSG00000024431 (Mm) , ENSRNOG00000014096 (Rn)

Orphanet

123916 (Hs)

Protein GI

121247453 (Mm) , 158303300 (Rn) , 324021685 (Hs)

NURSA Receptor

10.1621/R9FQ7TRSOT (Hs)

DrugBank Target

P04150 (Hs)

CATH/Gene3D

3.30.50.10 (N/A)

ChEMBL Target

CHEMBL2034 (Hs) , CHEMBL3368 (Rn) , CHEMBL3144 (Mm)

关联配体

Ligand ID	7088
名称	methylprednisolone
别名	Medrol®
类别	Metabolite
学名	(6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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	Methylprednisolone is a corticosteroid. Marketed formulations may contain methylprednisolone acetate (PubChem CID 5877). Methylprednisolone has been reported to activate the TRPC5 ion channel . Methylprednisolone-induced activation of TRPC5 is long lasting, reversible and sensitive to the TRPC5 inhibitor .

参考文献

1. Beckmann H, Richter J, Hill K, Urban N, Lemoine H, Schaefer M. (2017) A benzothiadiazine derivative and methylprednisolone are novel and selective activators of transient receptor potential canonical 5 (TRPC5) channels.. Cell Calcium, 66 (13): (10-18). [PMID:28807145]