LGD-3303
目录号 : GC32403
LGD-3303是一种口服的非甾体选择性雄激素受体调节剂（SARM），与雄激素受体具有高亲和力（Ki=0.9nM）。
Cas No.:917891-35-1
Sample solution is provided at 25 µL, 10mM.
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LGD-3303 is an orally active, non-steroidal selective androgen receptor modulator (SARM) with high affinity for the androgen receptor (Ki=0.9nM)[1, 2]. LGD-3303 binds to the mineralocorticoid receptor, glucocorticoid receptor, and progesterone receptor with much lower affinity than to the androgen receptor (Ki=1261, 581, and 136nM, respectively)[3]. LGD-3303 was designed to selectively activate the androgen receptor (AR) signaling pathway in muscle and other tissues, aiming to maintain anabolic (muscle-building) effects while minimizing androgen-related side effects on tissues such as the prostate[4].
In vivo studies in Sprague-Dawley rats showed that oral administration of LGD-3303 (3 or 30mg/kg/day) for 7 days significantly enhanced sexual preference for males in female rats, but only in sexually experienced females[5].
References:
[1] Vajda E G, López F J, Rix P, et al. Pharmacokinetics and pharmacodynamics of LGD-3303, an orally available nonsteroidalselective androgen receptor modulator[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 328(2): 663.
[2] Zhang X, Sui Z. Deciphering the selective androgen receptor modulators paradigm[J]. Expert opinion on drug discovery, 2013, 8(2): 191-218.
[3] Vajda E G, Hogue A, Griffiths K N, et al. Combination treatment with a selective androgen receptor modulator q (SARM) and a bisphosphonate has additive effects in osteopenic female rats[J]. Journal of Bone and Mineral Research, 2009, 24(2): 231-240.
[4] Clarke B L, Khosla S. Modulators of androgen and estrogen receptor activity[J]. Critical Reviews™ in Eukaryotic Gene Expression, 2010, 20(4).
[5] Kudwa A E, López F J, McGivern R F, et al. A selective androgen receptor modulator enhances male-directed sexual preference, proceptive behavior, and lordosis behavior in sexually experienced, but not sexually naive, female rats[J]. Endocrinology, 2010, 151(6): 2659-2668.
LGD-3303是一种口服的非甾体选择性雄激素受体调节剂（SARM），与雄激素受体具有高亲和力（Ki=0.9nM）[1, 2]。LGD-3303与矿物质皮质醇受体、糖皮质醇受体和孕激素受体的结合亲和力远低于与雄激素受体的结合亲和力（分别为Ki=1261、581和136nM）[3]。LGD-3303被设计用于选择性激活肌肉和组织中的雄激素受体（AR）通路，以期在维持合成代谢（肌肉增长）效应的同时，尽可能减少对前列腺等组织的雄激素副作用[4]。
在体内，LGD-3303（3, 30mg/kg/day）通过口服处理SD大鼠7天，显著增强了雌性对雄性的性偏好，但仅限于有性经验的雌性[5]。
| Animal experiment [1]: | |
Animal models | Female Sprague Dawley rat |
Preparation Method | Animals were ovariectomized (OVX) and 1 week later randomly assigned to four groups. DHT was administered via a SILASTIC capsule filled with crystalline DHT, implanted subcutaneously in the mid-scapular region under isoflurane anesthesia. In all cases, hormone/drug treatment began 1 week after ovariectomy. All other groups received an empty SILASTIC capsule. LGD-3303 was administered at two doses (3 and 30mg/kg; 4mL/kg) via oral gavage. DHT-treated and sham-operated animals received only vehicle. Briefly, LGD-3303 treatment was administered once daily for 7 days, 5-6h after lights out, 20h before testing. Animals received a pre-test after one dose of LGD-3303 to familiarize them with the testing apparatus. Seven days after treatment onset (2 weeks after OVX), all subjects were tested for sexual preference. To provide sexual experience, 4 days after the second sexual preference test, these animals underwent two sexual behavior tests with a sexually active male. For the sexual behavior tests, all animals received a single injection of Estradiol benzoate (40μg/kg s.c. in oil) 48h before testing. On the day of the sexual behavior test, animals were injected with Progesterone (1mg/kg) 3-4h before testing. Sexual behavior tests were separated by 4 days. Four days after the second sexual behavior test, LGD-3303 treatment was restarted, and all subjects underwent a second series of sexual preference tests: a pre-test on day 1 and a scored sexual preference test 7 days after treatment initiation. |
Dosage form | 3, 30mg/kg/day; 7 days; p.o. |
Applications | LGD-3303 enhances sexual preference of females for males when the females have had previous sexual experience. |
References: | |
| Cas No. | 917891-35-1 | SDF | |
| Canonical SMILES | O=C1NC2=C(C3=C(N(CC(F)(F)F)C(CC)=C3C)C=C2)C(Cl)=C1 | ||
| 分子式 | C16H14ClF3N2O | 分子量 | 342.74 |
| 溶解度 | DMSO : 6 mg/mL (17.51 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9177 mL | 14.5883 mL | 29.1766 mL |
| 5 mM | 583.5 μL | 2.9177 mL | 5.8353 mL |
| 10 mM | 291.8 μL | 1.4588 mL | 2.9177 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet