| Cat. No. |
Product Name |
CAS No. |
Information |
| H8979 |
Vosilasarm
|
1182367-47-0 |
Vosilasarm(RAD140)is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). IC50 value: 7 nM (Ki, fot androgen receptor) Target: androgen receptor in vitro: RAD140 demonstrates excellent affinity for the androgen receptor (Ki = 7 nM) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM); RAD140 is a novel SARM with high affinity and specificity for AR, is orally available, and exhibits potent anabolic effects in rodents and nonhuman primates.in vivo: The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats and monkeys. RAD140 is also neuroprotective using the rat kainate lesion model. RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate. |
| H8857 |
Rezvilutamide
|
1572045-62-5 |
Rezvilutamide is a potnet androgen receptor inhibitor,inhibit prostate cancer in a more effective manner. |
| H8850 |
Ludaterone
|
124548-08-9 |
Ludaterone is a novel antiandrogen. |
| H8627 |
Rezvilutamide
|
1572045-62-5 |
Rezvilutamide (developmental code name SHR3680) is a selective androgen receptor antagonist with reduced brain distribution compared to the structurally related nonsteroidal antiandrogen enzalutamide.As of October 2020, rezvilutamide is in phase 3 clinical trials for prostate cancer.Other structural analogues of rezvilutamide besides enzalutamide include apalutamide and proxalutamide. |
| H6296 |
DJ-V-159
|
2253744-53-3 |
DJ-V-159 is a novel small molecule agonist of GPRC6A, dose-dependently stimulates cAMP production in GPRC6A expressing HEK-293 cells at 0.2 nM; demonstrated the greatest potency in stimulating insulin secretion in β-cells and lowering serum glucose in wild-type mice. |
| H5669 |
RU 58841
|
154992-24-2 |
A nonsteroidal, specific androgen receptor inhibitor; be useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenetic alopecia and hirsutism. |
| H5668 |
RD162
|
915087-27-3 |
RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM; suppresses growth and induces apoptosis in human prostate cancer cells in vitro, demonstrates greater relative affinity than the clinically used antiandrogen bicalutamide, reduces the efficiency of its nuclear translocation, and impairs both DNA binding to androgen response elements and recruitment of coactivators; induces tumor regression in mouse models of castration-resistant human prostate cancer. |
| H5667 |
Proxalutamide
|
1398046-21-3 |
A potent androgen receptor (AR) antagonist with ability to down regulate AR protein level in prostate cancer cells; more potently inhibits androgen binding with AR's ligand binding domain than Bicalutamide (11.4-fold) and MDV3100 (3.5-fold) in biochemical assay; demonstrates stronger potency to block AR function of gene transcription in CRPC cells; demonstrates good anti-tumor efficacy among hormone sensitive, CRPC and AR+ breast cancer animal models. |
| H5666 |
ORM-15341
|
1297537-33-7 |
The active main metabolite of ODM-201, a potent wt/mutant androgen receptor (AR) inhibitor; inhibits wtAR/AR(F876L) with IC50s of 25/51 nM respectively; suppresses androgen-induced cell proliferation more efficaciously than enzalutamide or ARN-509. |
| H5665 |
ODM-201
|
1297538-32-9 |
A potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM; inhibits wtAR/AR(F876L) with IC50 of 65/66 nM respectively, weak inhibition on AR(W741L) and AR(T877A); inhibits the nuclear translocation of AR and more efficaciously than enzalutamide or ARN-509 in VCaP cell line proliferation assay; reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model. |
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