Free shipping on all orders over $ 500

ACT-1004-1239

Cat. No. M21310
ACT-1004-1239  Structure
Size Price Availability Quantity
5mg USD 650  USD650 In stock
10mg USD 1020  USD1020 In stock
25mg USD 2100  USD2100 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

ACT-1004-1239 is a potent, selective, orally administered CXCR7 antagonist with an IC50 value of 3.2 nM.

Chemical Information
Molecular Weight 522.55
Formula C27H28F2N6O3
CAS Number 2178049-58-4
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Christine Huynh, et al. Front Pharmacol. Absorption, Metabolism, and Excretion of ACT-1004-1239, a First-In-Class CXCR7 Antagonist: In Vitro, Preclinical, and Clinical Data

[2] Christine Huynh, et al. Biomed Pharmacother. Target engagement of the first-in-class CXCR7 antagonist ACT-1004-1239 following multiple-dose administration in mice and humans

[3] Laetitia Pouzol, et al. FASEB J. ACT-1004-1239, a first-in-class CXCR7 antagonist with both immunomodulatory and promyelinating effects for the treatment of inflammatory demyelinating diseases

[4] Christine Huynh, et al. Clin Pharmacol Ther. A Multipurpose First-in-Human Study With the Novel CXCR7 Antagonist ACT-1004-1239 Using CXCL12 Plasma Concentrations as Target Engagement Biomarker

[5] Sylvia Richard-Bildstein, et al. J Med Chem. Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239

Related CXCR Products
FC131 TFA

FC131 TFA is a CXCR4 antagonist, inhibits [125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM.

CTCE-0214

CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog.

TC14012

TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM.

CXCR4 antagonist 4

CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).

Ac-Pro-Gly-Pro-OH

Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and can be used as CXCR2 agonist.

  Catalog
Abmole Inhibitor Catalog




Keywords: ACT-1004-1239 supplier, CXCR, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.