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 (Highly Recommended)
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
1 mg USD 260 In-stock
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

Top Publications Citing Use of Products

View All CXCR Isoform Specific Products:

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • 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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (19.14 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. 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
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Concentration
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Volume
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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

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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. 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
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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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