E6130


Catalog No. Size PriceQuantity
M14098-2 Contact sales@xcessbio.com for quotation $100

Description

E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.

Product information

CAS Number: 1427058-33-0

Molecular Weight: 556.06

Formula: C28H37ClF3N3O3

Chemical Name: 2-[(3S,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-({1-[(cyclohex-1-en-1-yl)methyl]piperidin-4-yl}carbamoyl)-4-methylpyrrolidin-3-yl]acetic acid

Smiles: C[C@H]1CN(C[C@@]1(CC(O)=O)C(=O)NC1CCN(CC1)CC1CCCCC=1)CC1=C(C=CC=C1Cl)C(F)(F)F

InChiKey: JTJKDYLEMNXXER-UZTOHYMASA-N

InChi: InChI=1S/C28H37ClF3N3O3/c1-19-15-35(17-22-23(28(30,31)32)8-5-9-24(22)29)18-27(19,14-25(36)37)26(38)33-21-10-12-34(13-11-21)16-20-6-3-2-4-7-20/h5-6,8-9,19,21H,2-4,7,10-18H2,1H3,(H,33,38)(H,36,37)/t19-,27+/m0/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : ≥ 250 mg/mL (449.59 mM).

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:

E6130 is an orally active and highly selective CX3CR1 modulator, inhibits the fractalkine-induced chemotaxis of human peripheral blood natural killer cells (IC50, 4.9 nM), and down-regulates CX3CR1 on the cell surface of CD56+ NK cells with an EC50 value of 5.2 nM. E6130 also shows agonistic activity via CX3CR1 with respect to GTPγS binding (EC50 = 133 nM) and β-arrestin recruitment (EC50 = 2.4 μM) in CX3CR1-expressing CHO-K1 membrane but show no antagonistic activity.

In Vivo:

E6130 (10 or 30 mg/kg, p.o.) reduces several inflammatory bowel disease-related parameters in a murine CD4+ CD45RBhigh T-cell-transfer colitis model and a murine oxazolone-induced colitis model.

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

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed