TLB 150 Benzoate  (Synonyms: RAD150)

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^[1][2][3].

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.

TLB 150 Benzoate (1%; peri-nerve injection; single dose) produces a sustained local anesthetic block of guinea pig sciatic nerve conduction in vivo, with 50% of animals recovering from paralysis at approximately 2 days^[1].
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.

497.93

C₂₇H₂₀ClN₅O₃

1208070-53-4

Solid

White to off-white

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

Room temperature in continental US; may vary elsewhere.

• [1]. Ross S, et al. Cyclization of three n-ω-haloalkyl-n-methylaminoaceto-2, 6-xyilidide derivatives in relation to their local anesthetic effect in vitro and in vivo. J. Pharmacol. Exp. Ther. 182(2):351-361.

  [2]. Ross SB, et al. Pharmacokinetics of haloalkylamines: cyclization and distribution in blood in vitro and in vivo. J Pharm Pharmacol. 1975;27(5):322-328.

  [3]. Miller CP. Selective androgen receptor modulators. United States, US20100041721. 2010-02-18.