2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. ACT-1004-1239

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

For research use only. We do not sell to patients.

ACT-1004-1239 Chemical Structure

ACT-1004-1239 Chemical Structure

CAS No. : 2178049-58-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 747 In-stock
Solution
10 mM * 1 mL in DMSO USD 747 In-stock
Solid
5 mg USD 650 In-stock
10 mg USD 1050 In-stock
25 mg USD 2150 In-stock
50 mg USD 3450 In-stock
100 mg USD 5400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

ACT-1004-1239 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ACT-1004-1239 is a potent, selective, orally active CXCR7 antagonist with an IC50 value of 3.2 nM[1][2].

IC50 & Target

CXCR7

 

In Vitro

ACT-1004-1239 inhibits human, dog, rat, mouse, guinea pig, macaque CXCR7 with IC50s of 3.2, 2.3, 3.1, 2.3, 0.6, 1.5 nM respectively[1].
ACT-1004-1239 (1-10 µM, 30 days) promotes oligodendrocyte precursor cell (OPC) differentiation by increasing CXCL12 levels[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ACT-1004-1239 Related Antibodies
In Vivo

ACT-1004-1239 (100 mg/kg, p.o.) increase of plasma CXCL12 concentration in naive male DBA/1 mice[1].
ACT-1004-1239 (100 mg/kg, p.o., twice daily) reduces disease severity in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[2].
ACT-1004-1239 (100 mg/kg, p.o., twice daily) increases myelination in the Cuprizone (HY-W115718)-induced demyelination model mice[2].
ACT-1004-1239 (10 mg/kg, p.o., rats) shows a Cmax of 600 ng/h/mL, Tmax of 0.5 h, F (%) of 35%[1].
ACT-1004-1239 (1 mg/kg, i.v., rats) shows a Vss of 3.6 L/kg, Cl of 70 mL/min/kg, T1/2 of 1.3 h[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[2]
Dosage: 10-100 mg/kg
Administration: p.o., twice daily
Result: Reduced clinical disease scores, and increases survival rate.
Increases plasma CXCL12 concentration.
Reduces the infiltration of neutrophils, monocytes, monocytes-derived cells (MdCs), plasmacytoid dendritic cells (pDCs), DCs, natural killer (NK) cells, NK T cells, B cells, and T cells.
Reduces the number of CXCR4-expressing leukocytes.
Molecular Weight

522.55

Formula

C27H28F2N6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1CN(CC2CC2)CC[C@@H]1NC(C3=NOC(C4=CC=C(F)C=C4F)=C3)=O)NC5(C6=NC=CC=N6)CC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (38.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9137 mL 9.5685 mL 19.1369 mL
5 mM 0.3827 mL 1.9137 mL 3.8274 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 1.67 mg/mL (3.20 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9137 mL 9.5685 mL 19.1369 mL 47.8423 mL
5 mM 0.3827 mL 1.9137 mL 3.8274 mL 9.5685 mL
10 mM 0.1914 mL 0.9568 mL 1.9137 mL 4.7842 mL
15 mM 0.1276 mL 0.6379 mL 1.2758 mL 3.1895 mL
20 mM 0.0957 mL 0.4784 mL 0.9568 mL 2.3921 mL
25 mM 0.0765 mL 0.3827 mL 0.7655 mL 1.9137 mL
30 mM 0.0638 mL 0.3189 mL 0.6379 mL 1.5947 mL
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ACT-1004-1239 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ACT-1004-12392178049-58-4CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsOPCCXCL12EAE modelInhibitorinhibitorinhibit

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