ACT-1004-1239
Based on 4 publication(s) in Google Scholar
ACT-1004-1239 is a potent, selective, orally active CXCR7 antagonist with an IC50 value of 3.2 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.81%
- CAS 番号: 2178049-58-4
- 分子式: C27H28F2N6O3
- 分子量:522.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 ACT-1004-1239
More
生物活性
製品説明
IC50 & Target
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CXCR7 |
体外実験
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. .
体内実験
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.
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Animal Model:Myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[2]
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Dosage:10-100 mg/kg
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Administration:p.o., twice daily
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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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2178049-58-4
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性状 Solid
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分子量 522.55
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分子式 C27H28F2N6O3
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Color White to off-white
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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J Cell Mol Med
Stromal Cell Derived Factor-1 Promotes Hepatic Insulin Resistance via Inhibiting Hepatocyte Lipophagy. [Abstract]2025 Jan;29(2):e70352. PMID: 39855896 -
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bioRxiv
Characterizing the SASP-Dependent Paracrine Spreading of Senescence Between Human Brain Cell Types. [Abstract]2026 Feb 12:2026.02.10.705129. PMID: 41726875
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 1.67 mg/mL (3.20 mM); Suspended solution; Need ultrasonic
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Richard-Bildstein S, et al. Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239. J Med Chem. 2020 Dec 24;63(24):15864-15882. [Content Brief]
[2]. Pouzol L, et al. ACT-1004-1239, a first-in-class CXCR7 antagonist with both immunomodulatory and promyelinating effects for the treatment of inflammatory demyelinating diseases. FASEB J. 2021 Mar;35(3):e21431. [Content Brief]
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 |
ACT-1004-1239 関連分類
HY-142617 関連分類
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