货号 | 产品名 | 中文名称 | 产品描述 |
---|---|---|---|
SJ-MX0483B | Bazedoxifene Acetate | 醋酸巴多昔芬 |
Bazedoxifene acetate (TSE-424 acetate) 是一种有口服活性的,非甾体、第三代选择性的雌激素受体调节剂 (SERM),对 ERα 和 ERβ 作用的 IC50 值分别为 26 nM 和 99 nM,可用于骨质疏松症的研究。Bazedoxifene acetate 也是一种 IL-6/GP130 蛋白相互作用抑制剂,可用于胰腺癌的研究。 |
SJ-MX0199 | 4-Hydroxytamoxifen (Afimoxifene) | (E/Z)-4-羟基他莫昔芬 |
4-Hydroxytamoxifen (Afimoxifene)是 (Z)-4-Hydroxytamoxifen 和 (E)-4-Hydroxytamoxifen 的消旋体。(E/Z)-4-Hydroxytamoxifen 是雌激素受体 (estrogen receptor) 调节剂,在乳腺癌的治疗和化学疗法中应用广泛。4-Hydroxytamoxifen (Afimoxifene)可激活intein-Cas9突变体的靶向修饰效率。 |
SJ-MX0483A | Bazedoxifene hydrochloride | 盐酸巴多昔芬 | Bazedoxifene hydrochloride (TSE-424 hydrochloride) 是一种有口服活性的,能透过血脑屏障的,非甾体、选择性的雌激素受体调节剂 (SERM),对 ERα 和 ERβ 作用的 IC50 值分别为 26 nM 和 99 nM,可用于骨质疏松症的研究。Bazedoxifene hydrochloride 也是一种 IL-6/GP130 蛋白相互作用抑制剂,可用于胰腺癌的研究。 |
SJ-MX3729 | GDC-0927 | GDC-0927, in postmenopausal women with estrogen receptor positive (ER+) HER2-negative metastatic breast cancer (BC). | |
SJ-MH0043 | Chlorotrianisene | 氯丁烯二烯 | Chlorotrianisene 是一种长效的非甾体雌激素,是一种口服活性雌激素受体调节剂。Chlorotrianisene 具有抗雌激素活性。Chlorotrianisene 还有效抑制 COX-1 并抑制全血中的血小板聚集。 |
SJ-MX2498 | (-)-(S)-Equol | (-)-(S)-Equol是雌激素受体β (estrogen receptor β) 的高亲和力配体。 | |
SJ-MX1665 | G-1 | G-1 是一个非甾体,高亲和力且有选择性的 GPR30 激动剂,其 Ki 值为 11 nM。 | |
SJ-MX4007 | Propyl pyrazole triol (PPT) | Propyl pyrazole triol (PPT) 是一种选择性的雌激素受体 α (ERα) 激动剂。Propyl pyrazole triol (PPT) 对 ERα 的相对结合亲和力 (ERα: 49%) 是雌激素受体 β (ERβ: 0.12%) 的 410 倍。 | |
SJ-MX1329 | GDC-9545 | Giredestrant (GDC-9545) 是一种非甾体雌激素受体 (ER) 配体,口服有效的,选择性 ER 拮抗剂。Giredestrant 可以在 ER 配体结合域内与雌二醇 (Estradiol) 竞争结合并诱导构象变化。Giredestrant 具有抗肿瘤活性。 | |
SJ-MH0046 | Dienestrol | 双烯雌酚;双烯熊酚 | Dienestrol is a synthetic, non-steroidal estrogen acting as an estrogen receptor agonist for the treatment of menopausal and postmenopausal symptoms. It is structurally related to stilbestrol. It is used, usually as the cream, in the treatment of menopausal and postmenopausal symptoms. It is an estrogen receptor agonist. Estrogens work partly by increasing a normal clear discharge from the vagina and making the vulva and urethra healthy. Using or applying an estrogen relieves dryness and soreness in the vagina, itching, redness, or soreness of the vulva. Conditions that are treated with vaginal estrogens include a genital skin condition (vulvar atrophy), inflammation of the vagina (atrophic vaginitis), and inflammation of the urethra (atrophic urethritis). |
SJ-MH0047 | Ethisterone | 炔孕酮 | Ethisterone (Aethisteron; Progestoral; NSC-9565; NSC9565) is a progestogen hormone and a synthetic contraceptive that is being developed as an anticancer agent for the treatment of prostate cancer. It is the first orally bioactive progestin, ethisterone (pregneninolone, 17α-ethynyltestosterone or 19-norandrostane), the 17α-ethynyl analog of testosterone. Ethisterone is a progestogen that counteracts estrogenic proliferative effects on the endometrium. Ethisterone (dose range: 40 μg-5 mg/day × 6) stimulates weight gain but has a rather weak effect on the sulphate pools and incorporation rates in mice. |
SJ-MH0051 | Hexestrol | Hexestrol (formerly HSDB2149; HSDB-2149; Cycloestrol; Hexoestrol; Erythrohexestrol; Sinestrol) is a synthetic ER (estrogen receptor) agonist which binds to ERα and ERβ with EC50s of 0.07 nM and 0.175 nM, respectively. It also acts as a microtubule polymerization inhibitor. | |
SJ-MH0056 | Quinestrol | 炔雌醇环戊醚 | Quinestrol是一种合成的雌激素,有潜力用于乳腺癌和前列腺癌的相关研究。 |
SJ-MX2250 | Mestranol | 美雌醇 | Mestranol (Ethinyl Estradiol 3 Methyl Ether; Devocin; Norquen; Ovastol), the 3-methyl ether of ethinyl estradiol, is a potent estrogen receptor agonist that has been used as an oral contraceptive. Mestranol is a prodrug of ethinylestradiol and is biologically inactive. It has to be activated through demethylation in the liver. |
SJ-MX2969 | Ospemifene | 奥培米芬 | Ospemifene (FC-1271a; FC1271a; Osphena) is an orally bioactive medication and a non-hormonal selective estrogen receptor modulator (SERM), used for the treatment of dyspareunia. It has been approved for managing dyspareunia – pain during sexual intercourse– encountered by some women, more often in those who are post-menopausal. Ospemifene is a selective estrogen receptor modulator (SERM) acting similarly to an estrogen on the vaginal epithelium, building vaginal wall thickness which in turn reduces the pain associated with dyspareunia. |
SJ-MX3841 | GSK-4716 | GSK4716 is a novel, potent and selective estrogen-related receptor beta/gamma (ERRβ and ERRγ) agonist. Treatment of differentiated skeletal muscle cells with the ERRbeta/gamma agonist (GSK4716) produced a significant increase in the expression of GRalpha (isoform D) protein. Quantitative RT-PCR (Q-RT-PCR) analysis after treatment with GSK4716, revealed induction of the mRNAs encoding the glucocorticoid receptor (GR), 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1), the enzyme that converts inactive cortisone to cortisol and hexose-6-phosphate dehydrogenase expression (H6PDH) that stimulates oxoreduction by 11beta-HSD1. Candidate based expression profiling also demonstrated the mRNAs encoding characterized GR target genes, including C/EBP, ApoD and Monoamine oxidase-A (MAO-A) are induced in GSK4716 treated cells. In concordance with these observations, siRNA-mediated suppression of the mRNA encoding ERRgamma (but not ERRalpha and beta) attenuated the expression of mRNAs encoding GR, 11betaHSD1 and GR target gene(s). Similarly, treatment with the ERRgamma (and ERalpha) antagonist diethylstilbestrol (DES) suppressed glucocorticoid responsive gene expression in skeletal muscle cells. Interestingly, we observed that GSK4716 trans-activated GRE-TK-LUC in a GR-dependent manner. This study highlights the regulatory crosstalk between ERRgamma and GR signaling in skeletal muscle cells, and suggests the ERRgamma agonist modulates the expression of critical genes that control GR signaling and glucocorticoid sensitive gene expression. | |
SJ-MH0065 | Estradiol valerianate | Estradiol valerianate is a synthetic ester used to treat menopausal symptoms and hormone deficiencies. | |
SJ-MH0066 | Estropipate | 雌酮硫酸酯哌嗪 | Estropipate 是雌激素的一种形式, 可用于更年期症状和骨质疏松症的研究。 |
SJ-MH0073 | Clomiphene citrate | 枸橼酸氯米芬 | Clomifene Citrate is a selective estrogen receptor modulator. |
SJ-MX2274 | AZD9496 | AZD9496 是有效,选择性的雌激素受体 (ERα) 拮抗剂,IC50 为 0.28 nM。AZD9496 是一种口服有效的选择性雌激素受体降解剂 (SERD)。 |