TLB 150 Benzoate
Based on 1 Customer Validation
TLB 150 Benzoate (RAD150) is a nonsteroidal androgen receptor modulator with an IC50 value of 0.13 μM. TLB 150 Benzoate spontaneously cyclizes under physiological conditions to form RAD 179, resulting in a persistent, reversible, and slow neuronal conduction blockade. TLB 150 Benzoate can be used for research on neurological diseases.
For research use only. We do not sell to patients.
- Purity : 98.3%
- CAS No.: 1208070-53-4
- Formula: C27H20ClN5O3
- Molecular Weight:497.93
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
In Vitro
TLB 150 Benzoate (5 mM) cyclizes to form RAD 179 in a pH 7.4 buffered ethanol solution at 37°C with a half-life of 40 minutes[1].
TLB 150 Benzoate (5 mM; 20 min) is taken up by intact Rana pipiens frog sciatic nerves, cyclizes to form RAD 179[1].
TLB 150 Benzoate (5 mM; 20 min) produces a slowly reversible local anesthetic block of intact Rana pipiens frog sciatic nerves, with 50% recovery of action potential amplitude occurring approximately seven hours after washing[1].
TLB 150 Benzoate (0.1 mM) forms RAD 179 inside rabbit and rat erythrocytes, which undergoes slow first-order efflux with half-lives of 9 h and 4.4 h respectively, and depolarization of rat erythrocyte membranes with potassium chloride increases efflux rate to a half-life of 2.7 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Rabbit[2] | 2.5 mg/kg | i.v. | 1.2 h |
In Vivo
TLB 150 Benzoate (2.5 mg/kg; i.v.; single dose) cyclizes to RAD 179 in rabbit blood in vivo, with RAD 150 eliminated rapidly and RAD 179 eliminated slowly[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:White rabbits (either sex, 2.5-4.5 kg)[2]
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Dosage:2.5 mg/kg
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Administration:i.v.; single dose
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Result:Exceeded RAD 179 concentration in blood during the first 30 minutes post-injection, then rapidly decreased.
Reached near the limit of detection in blood by 4 hours.
Disappeared from plasma with a half-life of 1.2 hours.
Disappeared from erythrocytes at the same rate as in plasma.
Chemical Information
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CAS No. 1208070-53-4
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Appearance Solid
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Molecular Weight 497.93
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Formula C27H20ClN5O3
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Color White to off-white
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SMILES
N#CC1=CC=C(N[C@@H](C2=NN=C(C3=CC=C(C#N)C=C3)O2)[C@@H](OC(C4=CC=CC=C4)=O)C)C(C)=C1Cl
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Synonyms
RAD150
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
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Data Sheet (276 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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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)