SMN2 modulator-1
SMN2 modulator-1 is a brain-penetrant survival motor neuron (SMN) modulator. SMN2 modulator-1 post-translationally stabilizes SMN protein and increases SMN protein levels independent of SMN2 transcription. SMN2 modulator-1 can be used for the research of spinal muscular atrophy[1].
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- CAS 番号: 1537150-15-4
- 分子式: C14H12ClFN2O2S
- 分子量:326.77
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.29 μM
Compound: 27
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Stabilization of human SMN protein expressed in HEK293 cells expressing SMN2 promoter after 24 hrs by luciferase reporter gene assay
Stabilization of human SMN protein expressed in HEK293 cells expressing SMN2 promoter after 24 hrs by luciferase reporter gene assay
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[PMID: 28481536] |
SMN2 modulator-1 (Compound 27) (0.29-30 μM; 24 h) potently activates SMN2 expression in SMN2 reporter cells with an EC50 of 0.29 μM, reaching 190% of control activity[1].
SMN2 modulator-1 (0.4-10 μM; 48 h) increases SMN protein levels in GM003813T SMA patient fibroblasts by approximately 2-fold at a 2 μM 48 h treatment, in a dose-dependent manner[1].
SMN2 modulator-1 has a kinetic solubility of 31 μM at pH 7.4, a mouse liver microsome half-life of 39 min, human liver microsome half-life of >120 min, and mouse plasma half-life of 326 min[1].
SMN2 modulator-1 (1-30 μM; 30 min-8 h) does not inhibit the proteasome or autophagy in HEK293 cells, nor does it inhibit HPV-16 E6 mediated p53 degradation in vitro, indicating its SMN-stabilizing effect is not due to global protein degradation inhibition[1].
SMN2 modulator-1 shows adequate intestinal permeability in the Caco-2 cell model, with an apical-to-basal Papp of 15 × 10-6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hTERT-immortalized SMA patient fibroblasts (GM003813T)
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Concentration:0.4 μM; 2 μM; 10 μM
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Incubation Time:48 h
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Result:Produced a dose-dependent increase in SMN protein levels.
Increased SMN protein levels to approximately 2-fold relative to DMSO control at 2 μM.
| Species | Dose | Route | Cmax | AUC0-∞ (Plasma) | Tmax (Plasma) | T1/2 (Plasma) | Cmax (Brain) | AUC0-∞ (Brain) | Tmax (Brain) | T1/2 (Brain) |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | i.p. | 7660 ng/mL | 34291 ng·h/mL | 0.5 h | 2.2 h | 13500 ng/mL | 51310 ng·h/mL | 0.5 h | 1.9 h |
| Mice[1] | 20 mg/kg | p.o. | 286 ng/mL | 1641 ng·h/mL | 0.5 h | 3.4 h | 446 ng/mL | 2223 ng·h/mL | 0.5 h | 2.8 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:mice (adult)[1]
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Dosage:20 mg/kg
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Administration:i.p. or p.o.; single dose
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Result:Reached a plasma Cmax of 7660 ng/mL, plasma AUC0-24h of 34291 ng·h/mL, plasma Tmax of 0.5 h, plasma T1/2 of 2.2 h, brain Cmax of 13500 ng/mL, brain AUC0-24h of 51310 ng·h/mL, brain Tmax of 0.5 h, brain T1/2 of 1.9 h, and a brain-to-plasma ratio of 1.5:1 following intraperitoneal dosing.
Reached a plasma Cmax of 286 ng/mL, plasma AUC0-24h of 1641 ng·h/mL, plasma Tmax of 0.5 h, plasma T1/2 of 3.4 h, brain Cmax of 446 ng/mL, brain AUC0-24h of 2223 ng·h/mL, brain Tmax of 0.5 h, brain T1/2 of 2.8 h, and a brain-to-plasma ratio of 1.4:1 following oral dosing.
化学情報
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CAS 番号 1537150-15-4
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分子量 326.77
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分子式 C14H12ClFN2O2S
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SMILES
O=C(C1=CC=C(C(Cl)=C1)F)NC2=NC=C(C3(CCC3)O)S2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
SMN2 modulator-1 関連分類
HY-124640 関連分類
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