SB 699551
目录号 : GC12524SB 699551是一种联苯甲胺衍生物，为一种强效且选择性的5-HT5A受体拮抗剂。
Cas No.:864741-95-7
Sample solution is provided at 25 µL, 10mM.
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SB 699551, a biphenylmethylamine derivative, is a potent and selective 5-HT5A receptor antagonist [1]. SB 699551 can inhibit the activity of the androgen receptor (AR), reduce the mRNA and protein levels of PSA, and downregulate the expression of the AR target gene FKBP5[2]. SB 699551 has been widely used to regulate the hypotensive state in mouse models[3].
In vitro, SB 699551 significantly inhibits the formation of cell spheroids in HCC1954 cells and MCF-7 cells within 72 hours, with IC50 values of 0.3μM and 0.2μM, respectively[4]. Treatment with 3μM SB 699551 for 24 hours resulted in a significant decrease in the cell viability of AMO1 sgRNA-CT cells[5].
In vivo, subcutaneous injection of a single dose of SB 699551 (0.3mg/kg) prevented forgetting and amnesia in rats[6]. Intrathecal injection of 10μl at a concentration of 10nmol/rat for 10 minutes can reduce the analgesic effect induced by serotonin in rats[7]. A single intraperitoneal injection of SB 699551 (3mg/kg) within 2 hours improved the cognitive impairment induced by ketamine and enhanced the cognitive flexibility of rats[8].
References:
[1] Corbett D F, Heightman T D, Moss S F, et al. Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry[J]. Bioorganic & medicinal chemistry letters, 2005, 15(18): 4014-4018.
[2] Itsumi M, Shiota M, Sekino Y, et al. High‐throughput screen identifies 5‐HT receptor as a modulator of AR and a therapeutic target for prostate cancer[J]. The Prostate, 2020, 80(11): 885-894.
[3] Sánchez-Maldonado C, López-Sánchez P, Anguiano-Robledo L, et al. GR-127935-sensitive Mechanism Mediating Hypotension in Anesthetized Rats: Are 5-HT: 5B: Receptors Involved?[J]. Journal of Cardiovascular Pharmacology, 2015, 65(4): 335-341.
[4] Gwynne W D, Shakeel M S, Girgis-Gabardo A, et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells[J]. BMC cancer, 2020, 20(1): 724.
[5] Du T, Song Y, Ray A, et al. Ubiquitin receptor PSMD4/Rpn10 is a novel therapeutic target in multiple myeloma[J]. Blood, The Journal of the American Society of Hematology, 2023, 141(21): 2599-2614.
[6] Aparicio-Nava L, Márquez-García L A, Meneses A. Effects of 5-HT5A receptor blockade on amnesia or forgetting[J]. Behavioural Brain Research, 2019, 357: 98-103.
[7] Muñoz-Islas E, Vidal-Cantú G C, Bravo-Hernández M, et al. Spinal 5-HT5A receptors mediate 5-HT-induced antinociception in several pain models in rats[J]. Pharmacology Biochemistry and Behavior, 2014, 120: 25-32.
[8] Nikiforuk A, Hołuj M, Kos T, et al. The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia[J]. Neuropharmacology, 2016, 105: 351-360.
SB 699551是一种联苯甲胺衍生物，为一种强效且选择性的5-HT5A受体拮抗剂[1]。SB 699551可抑制雄激素受体(AR)的活性，降低PSA的mRNA和蛋白水平，并下调AR靶基因FKBP5的表达[2]。SB 699551已广泛用于调控小鼠模型中的低血压状态[3]。
在体外，SB 699551在72小时内显著抑制了HCC1954细胞和MCF-7细胞中细胞球体的形成，IC50值分别为0.3μM和0.2μM[4]。用3μM的SB 699551处理24小时导致AMO1 sgRNA-CT细胞的细胞活力显著下降[6]。
在体内，单次皮下注射SB 699551（0.3mg/kg）可防止大鼠的遗忘和记忆缺失[6]。鞘内注射10μl浓度为10nmol/只的SB 699551 10分钟可降低5-羟色胺诱导的大鼠镇痛作用[7]。2小时内单次腹腔注射SB 699551（3mg/kg）改善了氯胺酮诱导的认知障碍并增强了大鼠的认知灵活性[8]。
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation Method | The MCF-7 cells were cultured in DMEM medium containing 10% fetal bovine serum (FBS) for 48 hours, and 1μg/ml doxycycline was added to the medium. Different concentrations of SB 699551 (3μM, 4μM, and 5μM) or the carrier were used to treat the cells for 24 hours. Then, the cell lysates were collected and the changes in protein phosphorylation levels in the cells were detected by immunoblotting. |
Reaction Conditions | 3μM, 4μM, and 5μM; 24h |
Applications | SX-682 treatment reduced the phosphorylation level of AKT at the serine residue 473 (S473), as well as the decreased in the phosphorylation of p70-S6 kinase 1 (S6K). |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Male Sprague-Dawley rats (weighing 200-250g) were housed in a standard environment with a temperature controlled at 21±1℃ and humidity controlled at 40-50%. The light/dark cycle was 12/12 hours (lights on at 6:00 am). The rats were housed in pairs and received mild food restriction for at least one week before the test (17 grams of feed pellets per day). 75 minutes before the test, 10mg/kg dose of ketamine or solvent control was subcutaneously injected (s.c.); 30 minutes before ketamine injection, SB 699551 (3mg/kg) was intraperitoneally injected (i.p.). The number of animals in each experimental group was n=6. Each rat received only one attentional set-shifting test. |
Dosage form | 3mg/kg for once; i.p. |
Applications | SB 699551 improved the cognitive deficit induced by ketamine and enhanced the cognitive flexibility of the rats. |
References: | |
| Cas No. | 864741-95-7 | SDF | |
| 化学名 | 3-cyclopentyl-N-(2-(dimethylamino)ethyl)-N-((4'-((phenethylamino)methyl)-[1,1'-biphenyl]-4-yl)methyl)propanamide dihydrochloride | ||
| Canonical SMILES | CN(CCN(C(CCC1CCCC1)=O)CC2=CC=C(C3=CC=C(CNCCC4=CC=CC=C4)C=C3)C=C2)C.Cl.Cl | ||
| 分子式 | C34H45N3O.2HCl | 分子量 | 584.66 |
| 溶解度 | <14.62mg/ml in DMSO; <5.85mg/ml in ethanol | 储存条件 | Store at 4°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 | 1.7104 mL | 8.552 mL | 17.104 mL |
| 5 mM | 342.1 μL | 1.7104 mL | 3.4208 mL |
| 10 mM | 171 μL | 855.2 μL | 1.7104 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。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet