L-771688
目录号 : GC33410
L-771688是一个选择性α1A-Adrenoceptor受体拮抗剂，Ki值为0.43±0.02nM。
Cas No.:200050-59-5
Sample solution is provided at 25 µL, 10mM.
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L-771688 is a highly selective α1A-Adrenoceptor antagonist with a Ki of 0.43±0.02 nM.
Specific [3H]L-771688 binding to cloned human α1A-Adrenoceptors is inhibited with high potency by subtype selective compounds, GG818 (Ki=0.026±0.002 nM) and L-771688 (Ki=0.052±0.008 nM) and subtype non-selective α1-adrenoceptor antagonists, prazosin (Ki=0.088±0.0.032 nM) and terazosin (Ki=1.8±0.65 nM). The relative amount of [3H]L-771688 (0.5 nM) binding in various rat tissue membranes is highest in submaxillary gland (9.5 pmol/g tissue), followed by brain (5.8 pmol/g tissue), vas deferens (4.3 pmol/g tissue), kidney (3.4 pmol/g tissue), heart (1.5 pmol/g tissue), urethra (1.1 pmol/g tissue) and prostate (0.88 pmol/g tissue). In contrast, low specific [3H]L-771688 binding is observed in rat urinary bladder (0.55 pmol/g tissue), liver (0.44 pmol/g tissue), aorta (0.11 pmol/g tissue) and spleen (0.11 pmol/g tissue)[1].
[1]. Chang RS, et al. In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist. Eur J Pharmacol. 2000 Dec 15;409(3):301-12.
Cell experiment: | [3H]L-771688 is prepared by a catalytic reduction of the precursor, L-797429, in the presence of tritium gas followed by preparative high pressure liquid chromatography. Receptor membranes are prepared for [3H]prazosin/[125I]HEAT binding assays. To measure [3H]L-771688 binding, 980 μL of membranes (cloning human α1A or rat tissues) are added to triplicate tubes containing 10 μL of dimethyl sulfoxide (DMSO) (for total binding) or phentolamine (10 μM final concentration, for nonspecific binding) or tested compounds (at the desiring final concentrations) and 10 μL of [3H]L-771688 (0.3 to 0.6 nM final concentration for routine studies and 10 pM to 5 nM for saturation assays). [3H]L-771688 is diluted in DMSO/methanol/water (1:1:2) from stock solution to minimize its loss to the wall of test tubes. The binding reaction is conducted at 25°C for 1 h or various time intervals in the association rate studies[1]. |
References: [1]. Chang RS, et al. In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist. Eur J Pharmacol. 2000 Dec 15;409(3):301-12. | |
| Cas No. | 200050-59-5 | SDF | |
| Canonical SMILES | O=C(C([C@H](C1=CC=C(F)C(F)=C1)N2C(NCCCN3CCC(C4=NC=CC=C4)CC3)=O)=C(COC)NC2=O)OC | ||
| 分子式 | C28H33F2N5O5 | 分子量 | 557.59 |
| 溶解度 | DMSO : ≥ 100 mg/mL (179.34 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 | 1.7934 mL | 8.9672 mL | 17.9343 mL |
| 5 mM | 0.3587 mL | 1.7934 mL | 3.5869 mL |
| 10 mM | 0.1793 mL | 0.8967 mL | 1.7934 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.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet