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RAD140 

Cat. No.: HY-14383 Purity: 99.53%
Handling Instructions

RAD140 is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. RAD140 shows good selectivity over other steroid hormone nuclear receptors.

For research use only. We do not sell to patients.

RAD140 Chemical Structure

RAD140 Chemical Structure

CAS No. : 1182367-47-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 250 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

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Description

RAD140 is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. RAD140 shows good selectivity over other steroid hormone nuclear receptors[1].

IC50 & Target

Ki: 7 nM (Androgen receptor)[1]

In Vitro

RAD140 (0-300 nM; pretreated for 1 hour) increases neuron viability against Aβ in a concentration-dependent manner[2].
RAD140 (100 nM; 1 hour) protects cultured neurons against apoptotic insults. RAD140 shows protective profiles of significantly protecting against neuronal death induced by Aβ and AAII, but not H2O2[2].
RAD140 (100 nM; 15 minutes) induces a significant increase in levels of phosphorylated but not total ERK in neuronal cultures[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and RAD140 also has good bioavailability in rats (F = 27-63%) and monkeys (65-75%)[1].
In castrated immature rats, RAD140 (0.03-0.3 mg/kg; for 11 days) stimulates the levator ani bulbocavernosus muscle weight and prostate weight[1].
A high dose of RAD140 (10 mg/kg, p.o.) actually antagonizes the effect of testosterone propionate (TP) at 1 mg/kg on the seminal vesicles but adds to the effect of TP on the levator ani muscle. The effective dose for achieving antagonism by RAD140 is 0.3-1 mg/kg (p.o.) for 1 mg/kg TP (s.c.). In the young castrate male rat model, RAD140 appears to be a potent and complete androgen agonist on the levator ani, but a weaker, partial antagonist on the seminal vesicle and possibly the prostate[1].
RAD140 is neuroprotective in vivo using the rat kainate lesion model. In experiments with gonadectomized, adult male rats, RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as demonstrated by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

393.83

Formula

C₂₀H₁₆ClN₅O₂

CAS No.

1182367-47-0

SMILES

ClC1=C(C)C(N[[email protected]]([H])([[email protected]@]([H])(O)C)C2=NN=C(O2)C3=CC=C(C#N)C=C3)=CC=C1C#N

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 : ≥ 100 mg/mL (253.92 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5392 mL 12.6958 mL 25.3917 mL
5 mM 0.5078 mL 2.5392 mL 5.0783 mL
10 mM 0.2539 mL 1.2696 mL 2.5392 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

RAD140RAD 140RAD-140Androgen ReceptorandrogenoralneuroprotectiveneuronalInhibitorinhibitorinhibit

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