TR-100
Based on 1 Customer Validation
TR-100 is a Tpm3.1 inhibitor that binds to and disrupts Tpm3.1-containing Actin filaments, enhancing the depolymerizing effect of Tpm3.1 on actin without altering actin-tropomyosin binding. TR-100 induces actin cytoskeleton rearrangement. TR-100 shortens membrane nanotubes and alters tube thickness in a concentration-dependent manner. TR-100 increases basal insulin secretion and inhibits glucose-stimulated insulin secretion. TR-100 inhibits insulin-stimulated glucose uptake. TR-100 can be used for research on B lymphoma.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.0%
- CAS No.: 1128165-86-5
- 화학식: C26H38N4O
- 분자량:422.61
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | IC50 |
10.8 μM
Compound: 12420
|
Inhibition of dynamin 1-mediated endocytosis internalization of Tf-A594 in human U2OS cells pretreated for 30 mins
Inhibition of dynamin 1-mediated endocytosis internalization of Tf-A594 in human U2OS cells pretreated for 30 mins
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[PMID: 19459681] |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIN6 β-cells
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Concentration:25 µM (TR100); 2.8 mM or 25 mM (glucose)
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Incubation Time:1 h (TR100); 10-30 min after glucose stimulation (fixation)
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Result:Led to significant loss of F-actin at the cell cortex in both basal and glucose-stimulated states.
In Vivo
In Tpm3.1 knockout mice, TR-100 (40 mg/kg BW; i.p.; single injection; 1 h before GTT/ITT) has reduced impact on glucose clearance and does not suppress glucose-stimulated insulin secretion, consistent with on-target Tpm3.1 action[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type (10-12-week-old male)[2]
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Dosage:40 mg/kg BW
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Administration:i.p.; single injection; 1 h before GTT/ITT
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Result:Had blood glucose similar to vehicle-injected controls one hour after injection.
Decreased glucose clearance.
Suppressed glucose-stimulated insulin secretion completely; insulin levels were not different from baseline at all time points after glucose injection.
Had no impact on insulin-stimulated glucose clearance in the ITT.
Had little effect on glucose clearance at 8 h after administration.
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Animal Model:B6-Tpm3tm2(∆9d)Pgun (10-12-week-old male)[2]
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Dosage:40 mg/kg BW
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Administration:i.p.; single injection; 1 h before GTT/ITT
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Result:Decreased glucose clearance, but the impact was less than in wild-type mice.
Showed glucose-stimulated insulin secretion equivalent to vehicle controls.
Had no impact on insulin-stimulated glucose clearance in the ITT.
Chemical Information
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CAS No. 1128165-86-5
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Appearance Solid
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분자량 422.61
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화학식 C26H38N4O
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Color White to light yellow
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SMILES
O=C(NCCCCCCCC)/C(C#N)=C/C1=C(C)N(CCCN(C)C)C2=C1C=CC=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TR-100 Related Classifications
HY-124689 Related Classifications
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