CYM 50358 hydrochloride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。
Sample solution is provided at 25 µL, 10mM.
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CYM 50358 hydrochloride is a potent and selective sphingosine-1-phosphate receptor 4 (S1P4) antagonist, functioning by blocking the S1P₄ receptor. CYM 50358 hydrochloride can be employed for research on immunomodulatory mechanisms[1-2].
In vitro, CYM 50358 hydrochloride (10µM) was used to pretreat human platelets for 15 minutes, followed by stimulation with collagen (1µg/ml) for 4 minutes. CYM 50358 hydrochloride did not significantly affect collagen-induced HSP27 phosphorylation but reversed sphingosine-1-phosphate (S1P)-induced inhibition of HSP27 phosphorylation[3]. CYM 50358 hydrochloride (1µM) was used to pretreat murine C2C12 myoblasts for 30 minutes, followed by treatment with TGFβ1 (5ng/ml) for 18-24 hours. CYM 50358 hydrochloride significantly attenuated TGFβ1-induced caspase-3 activation and PARP cleavage[4].
In vivo, CYM 50358 hydrochloride (5mg/kg) was administered via intraperitoneal injection 30 minutes before OVA sensitization or 30 minutes after OVA challenge in female BALB/c mice. CYM 50358 hydrochloride 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]. CYM 50358 hydrochloride (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. CYM 50358 hydrochloride 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.
CYM 50358 hydrochloride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。CYM 50358 hydrochloride可被用于免疫调节机制的相关研究[1-2]。
在体外，CYM 50358 hydrochloride（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，CYM 50358 hydrochloride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]。CYM 50358 hydrochloride（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。CYM 50358 hydrochloride可显著减弱TGFβ1诱导的caspase-3活化与PARP裂解[4]。
在体内，CYM 50358 hydrochloride（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。CYM 50358 hydrochloride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]。CYM 50358 hydrochloride（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。CYM 50358 hydrochloride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. CYM 50358 hydrochloride (1μM) was incubated 30 min before the first agonist addition. |
Reaction Conditions | 1μM; 30min pretreatment before TGFβ1 stimulation for 24h. |
Applications | CYM 50358 hydrochloride pretreatment appreciably reduced the stimulation of caspase-3 activity and the cleavage of PARP elicited by TGFβ1. CYM 50358 hydrochloride 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. CYM 50358 hydrochloride (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 | CYM 50358 hydrochloride 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. | SDF | ||
| 化学名 | (Z)-N-(4-(aminomethyl)-2,6-dimethylphenyl)-5-(2,5-dichlorophenyl)furan-2-carbimidic acid hydrochloride | ||
| Canonical SMILES | CC1=C(/N=C(O)/C2=CC=C(O2)C3=C(Cl)C=CC(Cl)=C3)C(C)=CC(CN)=C1.Cl | ||
| 分子式 | C20H18Cl2N2O2.HCl | 分子量 | 425.74 |
| 溶解度 | <42.57mg/ml in DMSO; <42.57mg/ml in Water | 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 | 2.3489 mL | 11.7443 mL | 23.4885 mL |
| 5 mM | 469.8 μL | 2.3489 mL | 4.6977 mL |
| 10 mM | 234.9 μL | 1.1744 mL | 2.3489 mL |
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| 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 |
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| % 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，
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1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >97.00% Appearance: A solid
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