CE-224535


Catalog No. Size PriceQuantity
M20173-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

CE-224535 is a selective P2X7 receptor antagonist.

Product information

CAS Number: 724424-43-5

Molecular Weight: 480.94

Formula: C22H29ClN4O6

Chemical Name: 2-chloro-5-{4-[(2R)-2-hydroxy-3-methoxypropyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazin-2-yl}-N-[(1-hydroxycycloheptyl)methyl]benzamide

Smiles: COC[C@H](O)CN1C(=O)C=NN(C2C=C(C(Cl)=CC=2)C(=O)NCC2(O)CCCCCC2)C1=O

InChiKey: FUCKCIVGBCBZNP-MRXNPFEDSA-N

InChi: InChI=1S/C22H29ClN4O6/c1-33-13-16(28)12-26-19(29)11-25-27(21(26)31)15-6-7-18(23)17(10-15)20(30)24-14-22(32)8-4-2-3-5-9-22/h6-7,10-11,16,28,32H,2-5,8-9,12-14H2,1H3,(H,24,30)/t16-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

CE-224535 is developed as a disease-modifying antirheumatic drugs (DMARD) and is a selective antagonist of the human P2X7 receptor. CE-224535 can reduce leukocyte secretion of IL-1 and IL-18, thereby providing a novel therapeutic approach for treatment of rheumatoid arthritis (RA).

In Vivo:

In rats, CE-224535 has low CLp (11 mL/min/kg) and a large Vdss of 7.6 L/kg, which results in a half-life of 2.4 h. Upon oral administration to rats at 5 mg/kg, CE-224535 provides maximal plasma exposure (Cmax) that is ~90 fold over its IC90 in human blood (Cmax=0.21 μg/mL or 0.44 μM). The oral bioavailability of CE-224535 is low in rats (F=2.6%), but this is believed to be a rat specific phenomenon since corresponding oral bioavailability in both dog (59%) and monkey (22%) is adequate.

Products are for research use only. Not for human use.

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