Home >> Research Area >>GPCR/G protein>>CCR2>> INCB8761(PF-4136309)

INCB8761(PF-4136309)

CAS# 1341224-83-6

INCB8761(PF-4136309)

Catalog No. BCC1649----Order now to get a substantial discount!

Product Name & Size Price Stock
INCB8761(PF-4136309): 5mg $414 In Stock
INCB8761(PF-4136309): 10mg Please Inquire In Stock
INCB8761(PF-4136309): 20mg Please Inquire Please Inquire
INCB8761(PF-4136309): 50mg Please Inquire Please Inquire
INCB8761(PF-4136309): 100mg Please Inquire Please Inquire
INCB8761(PF-4136309): 200mg Please Inquire Please Inquire
INCB8761(PF-4136309): 500mg Please Inquire Please Inquire
INCB8761(PF-4136309): 1000mg Please Inquire Please Inquire
Related Products

Quality Control of INCB8761(PF-4136309)

Number of papers citing our products

Chemical structure

INCB8761(PF-4136309)

3D structure

Chemical Properties of INCB8761(PF-4136309)

Cas No. 1341224-83-6 SDF Download SDF
PubChem ID 11192346 Appearance Powder
Formula C29H31F3N6O3 M.Wt 568.59
Type of Compound N/A Storage Desiccate at -20°C
Synonyms INCB8761
Solubility DMSO : ≥ 34 mg/mL (59.80 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[2-[(3S)-3-[[4-hydroxy-4-(5-pyrimidin-2-ylpyridin-2-yl)cyclohexyl]amino]pyrrolidin-1-yl]-2-oxoethyl]-3-(trifluoromethyl)benzamide
SMILES C1CC(CCC1NC2CCN(C2)C(=O)CNC(=O)C3=CC(=CC=C3)C(F)(F)F)(C4=NC=C(C=C4)C5=NC=CC=N5)O
Standard InChIKey ZNSVOHSYDRPBGI-CBQRAPNFSA-N
Standard InChI InChI=1S/C29H31F3N6O3/c30-29(31,32)21-4-1-3-19(15-21)27(40)36-17-25(39)38-14-9-23(18-38)37-22-7-10-28(41,11-8-22)24-6-5-20(16-35-24)26-33-12-2-13-34-26/h1-6,12-13,15-16,22-23,37,41H,7-11,14,17-18H2,(H,36,40)/t22?,23-,28?/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of INCB8761(PF-4136309)

DescriptionPF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50 of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.In Vitro:PF-4136309 is potent in human chemotaxis activity (IC50=3.9 nM) and in the whole blood assay (IC50=19 nM), with IC50 of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC50 values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC50 of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC50 values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM[1].In Vivo:PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (Tmax) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species[1].

References:
[1]. Xue CB, et al. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. ACS Med. Chem. Lett., 2011, 2 (12), pp 913-918.

INCB8761(PF-4136309) Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

INCB8761(PF-4136309) Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of INCB8761(PF-4136309)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7587 mL 8.7937 mL 17.5874 mL 35.1747 mL 43.9684 mL
5 mM 0.3517 mL 1.7587 mL 3.5175 mL 7.0349 mL 8.7937 mL
10 mM 0.1759 mL 0.8794 mL 1.7587 mL 3.5175 mL 4.3968 mL
50 mM 0.0352 mL 0.1759 mL 0.3517 mL 0.7035 mL 0.8794 mL
100 mM 0.0176 mL 0.0879 mL 0.1759 mL 0.3517 mL 0.4397 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on INCB8761(PF-4136309)

INCB8761(PF-4136309) is a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Featured Products
New Products
 

References on INCB8761(PF-4136309)

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.[Pubmed:24900280]

ACS Med Chem Lett. 2011 Oct 5;2(12):913-8.

We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, high selectivity, weak hERG activity, and an excellent in vitro and in vivo ADMET profile. INCB8761/PF-4136309 has entered human clinical trials.

Description

PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.

Keywords:

INCB8761(PF-4136309),1341224-83-6,INCB8761,Natural Products,CCR2, buy INCB8761(PF-4136309) , INCB8761(PF-4136309) supplier , purchase INCB8761(PF-4136309) , INCB8761(PF-4136309) cost , INCB8761(PF-4136309) manufacturer , order INCB8761(PF-4136309) , high purity INCB8761(PF-4136309)

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: