CYM50358是一种有效的、选择性的鞘氨醇-1-磷酸4（S1P4）受体拮抗剂，通过拮抗S1P4受体发挥作用。
Cas No.:1314212-39-9
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
CYM50358 is a potent and selective sphingosine-1-phosphate receptor 4 (S1P4) antagonist, functioning by blocking the S1P₄ receptor. CYM50358 can be employed for research on immunomodulatory mechanisms[1-2].
In vitro, CYM50358 (10µM) was used to pretreat human platelets for 15 minutes, followed by stimulation with collagen (1µg/ml) for 4 minutes. CYM50358 did not significantly affect collagen-induced HSP27 phosphorylation but reversed sphingosine-1-phosphate (S1P)-induced inhibition of HSP27 phosphorylation[3]. CYM50358 (1µM) was used to pretreat murine C2C12 myoblasts for 30 minutes, followed by treatment with TGFβ1 (5ng/ml) for 18-24 hours. CYM50358 significantly attenuated TGFβ1-induced caspase-3 activation and PARP cleavage[4].
In vivo, CYM50358 (5mg/kg) was administered via intraperitoneal injection 30 minutes before OVA sensitization or 30 minutes after OVA challenge in female BALB/c mice. CYM50358 significantly inhibited the increase of eosinophils and lymphocytes in bronchoalveolar lavage fluid, reduced lung inflammation scores, suppressed mucin secretion, and lowered serum IgE and IL-4 levels[5]. CYM50358 (2.5mg/kg) was administered via intraperitoneal injection every two days starting from day 3 after rhesus rotavirus (RRV) injection until day 14 in neonatal Balb/c mice. CYM50358 significantly improved RRV-induced biliary atresia, reduced the incidence of extrahepatic biliary obstruction, alleviated liver inflammation and fibrosis, improved liver function, and increased survival rates[6].
References:
[1] Podolak I, Janeczko Z, Galanty A, et al. A triterpene saponin from Lysimachia thyrsiflora L. Acta Pol Pharm. 2007 Jan-Feb;64(1):39-43.
[2] Kitada Y, Kajita K, Taguchi K, et al. Blockade of Sphingosine 1-Phosphate Receptor 2 Signaling Attenuates High-Fat Diet-Induced Adipocyte Hypertrophy and Systemic Glucose Intolerance in Mice. Endocrinology. 2016 May;157(5):1839-51.
[3] Onuma T, Tanabe K, Kito Y, et al. Sphingosine 1-phosphate (S1P) suppresses the collagen-induced activation of human platelets via S1P4 receptor. Thromb Res. 2017 Aug;156:91-100.
[4] J Cencetti F, Bernacchioni C, Tonelli F, et al. TGFβ1 evokes myoblast apoptotic response via a novel signaling pathway involving S1P4 transactivation upstream of Rho-kinase-2 activation. FASEB J. 2013 Nov;27(11):4532-46.
[5] Jeon WJ, Chung KW, Lee JH, et al. Suppressive Effect of CYM50358 S1P4 Antagonist on Mast Cell Degranulation and Allergic Asthma in Mice. Biomol Ther (Seoul). 2021 Sep 1;29(5):492-497.
[6] Sun D, Wang D, Jia L, et al. S1P/S1PR4 promotes the differentiation of CD8+ tissue-resident memory T cells aggravating bile duct injury in biliary atresia. J Hepatol. 2026 Feb;84(2):385-398.
CYM50358是一种有效的、选择性的鞘氨醇-1-磷酸4（S1P4）受体拮抗剂，通过拮抗S1P4受体发挥作用。CYM50358可被用于免疫调节机制的相关研究[1-2]。
在体外，CYM50358（10μM）预处理人血小板15分钟，随后以胶原蛋白（1μg/ml）刺激4分钟，CYM50358对胶原诱导的HSP27磷酸化无显著影响，但可逆转鞘氨醇-1-磷酸（S1P）诱导的HSP27磷酸化抑制[3]。CYM50358（1μM）预处理鼠C2C12成肌细胞30分钟，随后以TGFβ1（5ng/ml）处理18-24小时。CYM50358可显著减弱TGFβ1诱导的caspase-3活化与PARP裂解[4]。
在体内，CYM50358（5mg/kg）在OVA致敏前30分钟或OVA激发后30分钟经腹腔注射，用于处理雌性BALB/c小鼠。CYM50358显著抑制了支气管肺泡灌洗液中嗜酸性粒细胞和淋巴细胞的增加、肺部炎症评分、黏蛋白分泌以及血清IgE和IL-4水平的升高[5]。CYM50358（2.5mg/kg）在rhesus rotavirus（RRV）后第3天开始，每2天一次腹腔注射，用于处理新生Balb/c小鼠直至第14天。CYM50358显著改善了RRV诱导的胆道闭锁、降低了肝外胆道阻塞发生率、减轻了肝脏炎症和纤维化、改善了肝功能并提高了生存率[6]。
| Cell experiment [1]: | |
Cell lines | C2C12 myoblasts (mouse skeletal muscle cell line) |
Preparation Method | C2C12 myoblasts were serum-starved and then treated with TGFβ1 (5ng/ml) 30 min and 18 h after starvation. CYM50358 (1μM) was incubated 30 min before the first agonist addition. |
Reaction Conditions | 1μM; 30min pretreatment before TGFβ1 stimulation for 24h. |
Applications | CYM50358 pretreatment appreciably reduced the stimulation of caspase-3 activity and the cleavage of PARP elicited by TGFβ1. CYM50358 also enhanced the extent of Akt phosphorylation in response to S1P treatment in TGFβ1-treated myoblasts. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | Female 6-week-old BALB/c mice were randomly assigned to an OVA-induced allergic asthma model. CYM50358 (5mg/kg) was administered via intraperitoneal injection 30 minutes before OVA sensitization (on day 0 and 14) or 30 minutes before OVA challenge (on days 28, 29, and 30). Bronchoalveolar lavage fluid (BALF) and lung tissues were collected on day 32 for analysis. |
Dosage form | 5mg/kg; i.p.; administered 30min before sensitization or challenge. |
Applications | CYM50358 administration significantly inhibited the OVA-induced increase of total cells, eosinophils, and lymphocytes in BALF, reduced lung inflammation scores, suppressed mucin production (PAS-positive cells), and decreased serum IgE and BALF IL-4 levels. |
References: | |
| Cas No. | 1314212-39-9 | SDF | |
| 分子式 | C20H18Cl2N2O2 | 分子量 | 389.28 |
| 溶解度 | DMSO : 125 mg/mL (321.11 mM; Need ultrasonic) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5688 mL | 12.8442 mL | 25.6885 mL |
| 5 mM | 513.8 μL | 2.5688 mL | 5.1377 mL |
| 10 mM | 256.9 μL | 1.2844 mL | 2.5688 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet