BLT-1是一种选择性的清道夫受体B类I型（SR-BI）抑制剂，可抑制DiI标记的高密度脂蛋白（HDL）摄取，IC50值为0.021μM。
Cas No.:321673-30-7
Sample solution is provided at 25 µL, 10mM.
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BLT-1 is a selective scavenger receptor B, type 1 (SR-BI) inhibitor that inhibits DiI-labeled high-density lipoprotein (HDL) uptake with an IC50 value of 0.021μM [1]. BLT-1 blocks lipid transport, including selective uptake and efflux, to prevent SR-BI-mediated cholesterol efflux from cells to HDL[2]. BLT-1 has been widely used to prevent hepatitis C virus (HCV) infection of cells and enhance viral clearance [3].
In vitro, BLT-1 treatment for 3 hours significantly inhibited the proliferation of MCF-7 and MDA-MB-468 cells with the IC50 values of 55nM and 48nM, respectively[4]. Treatment with 10μM BLT-1 for 24 hours in HUVECs enhanced the pro-inflammatory effect induced by sphingosine-1-phosphate (S1P), accompanied by an increase in the protein levels of TNF-α and IL-1β[5]. BLT-1 (10μM) combined with SR-BI siRNA pretreatment for 2 hours on THP-1 macrophages significantly inhibited baicalin-induced cholesterol efflux[6].
In vivo, BLT-1 treatment (25mg/kg/day; p.o.) for 15 days can lead to higher levels of lipid peroxides in the acute myeloid leukemia model of mice, thereby inhibiting the progression of leukemia through ferroptosis[7]. Oral administration of 25mg/kg dose of BLT-1 daily for 4 consecutive weeks inhibited the tumor growth in a PC3 cell-xenograft mouse model, without affecting the body weight [8].
References:
[1] Nieland T J F, Shaw J T, Jaipuri F A, et al. Identification of the molecular target of small molecule inhibitors of HDL receptor SR-BI activity[J]. Biochemistry, 2008, 47(1): 460-472.
[2] Nieland T J F, Penman M, Dori L, et al. Discovery of chemical inhibitors of the selective transfer of lipids mediated by the HDL receptor SR-BI[J]. Proceedings of the national academy of sciences, 2002, 99(24): 15422-15427.
[3] Ohashi H, Koizumi Y, Fukano K, et al. Reply to Padmanabhan and Dixit: Hepatitis C virus entry inhibitors for optimally boosting direct-acting antiviral-based treatments[J]. Proceedings of the National Academy of Sciences, 2017, 114(23): E4527-E4529.
[4] Karimi N, Tehrani F S K. Expression of SR-B1 receptor in breast cancer cell lines, MDAMB-468 and MCF-7: Effect on cell proliferation and apoptosis[J]. Iranian Journal of Basic Medical Sciences, 2021, 24(8): 1069.
[5] Ren K, Lu Y J, Mo Z C, et al. ApoA-I/SR-BI modulates S1P/S1PR2-mediated inflammation through the PI3K/Akt signaling pathway in HUVECs[J]. Journal of physiology and biochemistry, 2017, 73(2): 287-296.
[6] Yu R, Lv Y, Wang J, et al. Baicalin promotes cholesterol efflux by regulating the expression of SR-BI in macrophages[J]. Experimental and Therapeutic Medicine, 2016, 12(6): 4113-4120.
[7] Shi J, Cheng Y, Wang L, et al. SR-B1 deficiency suppresses progression in acute myeloid leukemia via ferroptosis and reverses resistance to venetoclax[J]. Free Radical Biology and Medicine, 2025, 233: 24-38.
[8] Gordon J A, Noble J W, Midha A, et al. Upregulation of scavenger receptor B1 is required for steroidogenic and nonsteroidogenic cholesterol metabolism in prostate cancer[J]. Cancer research, 2019, 79(13): 3320-3331.
BLT-1是一种选择性的清道夫受体B类I型（SR-BI）抑制剂，可抑制DiI标记的高密度脂蛋白（HDL）摄取，IC50值为0.021μM[1]。BLT-1阻断脂质转运，包括选择性摄取和外排，从而阻止SR-BI介导的胆固醇从细胞外流至HDL[2]。BLT-1已被广泛用于预防丙型肝炎病毒（HCV）感染细胞并增强病毒清除[3]。
在体外，BLT-1处理3小时显著抑制了MCF-7和MDA-MB-468细胞的增殖，IC50值分别为55nM和48nM[4]。在HUVEC细胞中使用10μM的BLT-1处理24小时，增强了1-磷酸鞘氨醇（S1P）诱导的促炎效应，并伴有TNF-α和IL-1β蛋白水平的升高[5]。BLT-1（10μM）联合SR-BI siRNA预处理THP-1巨噬细胞2小时，显著抑制了baicalin诱导的胆固醇外流[6]。
在体内，每日口服给予BLT-1（25mg/kg），持续15天，可导致小鼠急性髓系白血病模型中脂质过氧化物水平升高，从而通过铁死亡抑制白血病的进展[7]。连续4周每日口服25mg/kg剂量的BLT-1，抑制了PC3细胞异种移植小鼠模型中的肿瘤生长，且未影响体重[8]。
| Cell experiment [1]: | |
Cell lines | MDA-MB-468 cells |
Preparation Method | MDA-MB-468 cells were cultured in RPMI 1640 medium supplemented with 10% (v/v) FCF, 100µg/ml streptomycin and 100U/ml penicillin in an incubator at 37℃, 100% humidity and 5% CO2. 7.5×103 cells in 200µl/well were added to 96-well plates, and after overnight cell attachment, the cells were stimulated with different concentrations of BLT-1 (15, 30, 50, 100, and 200nM) for 1, 3, and 5h to analyze cell viability. |
Reaction Conditions | 15, 30, 50, 100, and 200nM; 1, 3, and 5h |
Applications | BLT-1 treatment decreased the cell viability of MDA-MB-468 cells in a dose- and time-dependent fashion. |
| Animal experiment [2]: | |
Animal models | Athymic nude mice (Crl:NU-Foxn1nu) |
Preparation Method | Athymic nude mice (Crl:NU-Foxn1nu) were housed in a specific pathogen-free (SPF) animal house at 24±2°C temperature and 55±5% humidity and maintained on a 12h light/12h dark circadian rhythm. A total of 2×106 PC3 cells were inoculated subcutaneously on the hind flank of athymic nude mice. Once tumors exceeded 100mm3, mice were randomized into vehicle (propylene glycol) or 25mg/kg BLT-1 treatment (by oral gavage) cohorts administered daily for 4 weeks. Tumor volumes (TV) were measured using calipers and the equation TV=length×width×height×0.5326. |
Dosage form | 25mg/kg/day for 4 weeks; p.o. |
Applications | BLT-1 treatment suppressed PC3 tumor growth in mice without affecting body weight. |
References: | |
| Cas No. | 321673-30-7 | SDF | |
| 别名 | Block lipid transport-1 | ||
| Canonical SMILES | CCCCCCC1CCC/C1=N/NC(N)=S | ||
| 分子式 | C12H23N3S | 分子量 | 241.4 |
| 溶解度 | DMSO: 41.67 mg/mL (172.62 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 4.1425 mL | 20.7125 mL | 41.425 mL |
| 5 mM | 828.5 μL | 4.1425 mL | 8.285 mL |
| 10 mM | 414.3 μL | 2.0713 mL | 4.1425 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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