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  4. Amiselimod

Amiselimod (MT-1303) 在体内通过鞘氨醇激酶转化为其活性磷酸代谢产物 Amiselimod phosphate。Amiselimod 是一种具有口服活性，高选择性的鞘氨醇 1-磷酸受体 1 (S1P1) 激动剂，旨在减少与芬戈莫德和其他 S1P 受体调节剂相关的心动过缓效应。Amiselimod 通过抑制致结肠炎 Th 1和 Th17 细胞浸润结肠来抑制慢性结肠炎。Amiselimod 通过减少自身反应性 T 细胞浸润肾脏来抑制狼疮肾炎。Amiselimod 有望用于自身免疫性疾病的研究。

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Amiselimod

Amiselimod Chemical Structure

CAS No. : 942399-20-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Amiselimod (MT-1303) is converted to its active metabolite Amiselimod phosphate by sphingosine kinases in vivo. Amiselimod is an orally active and high selectivity sphingosine 1-phosphate receptor-1 (S1P1) agonist, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod inhibits chronic colitis via inhibiting infiltration of colitogenic Th1 and Th17 cells into the colon. Amiselimod inhibits lupus nephritis by reducing the infiltration of autoreactive T cells into the kidneys. Amiselimodis promising for research of autoimmune diseases[1][2][3][4].

体外研究
(In Vitro)

Amiselimod (100 nM, 12 h) 在 HEK293 细胞或原代 HCMs (人类心肌细胞) 中转化为Amiselimod-P 的速度比 Fingolimod (HY-11063) 转化为 fingolimod-P 的速度慢[1]。 Amiselimod-P (0.001-1000 nM) 在人 S1P1 受体表达细胞中表现出 S1P1 受体激动剂活性, EC50 为 75 pM, 其活性高于在 S1P4 和 S1P5 受体上的活性，但在 S1P2 或 S1P3 受体上没有明显的激动剂活性[1]。
Amiselimod-P (0.001-1000 nM) 在人类心房肌细胞中以浓度依赖的方式增加 G 蛋白激活的内向整流钾通道(GIRK) 电流幅度，其 EC50 值为 41.6 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Amiselimod 相关抗体:
体内研究
(In Vivo)

Amiselimod (p.o., 1 mg/kg) hydrochloride 在大鼠心脏组织中转化为 Amiselimod-P 的浓度低于 fingolimod-P，这可能是其对心脏影响较小的原因[1]。
Amiselimod (p.o., 1 mg/kg, 对照组和 0.3 mg/kg 之间间隔 6 天，剂量水平为 0.3、3 和 30 mg/kg 之间间隔 13 或 14 天) 在猴子体内对心率或心电图参数没有影响[1]。
Amiselimod (0.3 mg/kg, p.o., 每日一次, 连续 3 天) 可降低 C57BL/6 小鼠 肠系膜淋巴结 CD4+ 细胞上 S1P1 的表达[3]。
. Amiselimod (0.3 mg/kg, p.o., 每日一次, 连续 28 天) 抑制由CD4+CD45RBhighT 细胞过继转移诱导 SCID 小鼠结肠炎的发展[3]。
Amiselimod (0.3 mg/kg, p.o., 每日一次, 持续 3-4 周) 减少了 Th1 和 Th17 细胞向由CD4+CD45RB high T 细胞过继转移诱导结肠炎小鼠结肠的浸润[3]。
Amiselimod (0.1-0.3 mg/kg, p.o., 每日一次, 连续 21 天) 抑制慢性结肠炎的发展，与抗mTNF-αmAb (250 μg/只小鼠) 在过继转移 CD4+ CD45RBhighT 细胞诱导的结肠炎小鼠中的效果相当[3]。
Amiselimod (0.1-1 mg/kg, p.o., 每日一次, 连续 18 周) 显著抑制 MRL/lpr 小鼠狼疮性肾炎的发展[4]。
Amiselimod (0.1-0.3 mg/kg, p.o., 每日一次, 连续 10 周) 可阻止 NZBWF1 小鼠狼疮性肾炎的进展[4]。
Amiselimod (0.3 mg/kg, p.o., 每日一次, 连续 13 周) 减少 T 细胞向 NZBWF1 小鼠肾脏的浸润[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four male cynomolgus monkeys, Macaca fascicularis, 3-4 years old [1].
Dosage: 0.3, 3, 30 mg/kg
Administration: p.o., with a 6 day interval between vehicle and 0.3 mg/kg, 13 or 14 day intervals between dose levels of 0.3, 3 and 30 mg/kg.
Result: Had no effects on heart rate or ECG parameters, including PR interval, QRS duration, QT interval and QTc at doses up to 30 mg/kg
Did not affect blood pressure at doses up to 30 mg/kg.
Animal Model: Male C57BL/6 mice, aged 5 weeks[3].
Dosage: 0.3 mg/kg
Administration: p.o., daily, 3 days
Result: Decreased S1P1 expression on CD4+ T cells from mesenteric lymph nodes.
Animal Model: Immunodeficient SCID mice with chronic colitis induced by adoptive transfer of CD4+CD45RBhigh T cells from BALB/c mice[3].
Dosage: 0.1, 0.3 mg/kg
Administration: p.o., daily, 28 days
Result: Body weight remained higher than that in the control group from 4 days after cell transfer.
Body weight in the 0.3 mg/kg treated group was significantly higher than that in the control group from 17 days.
Clinical scores (sum of scores for hunching, wasting, colon thickening, and stool consistency) in the 0.1 and 0.3 mg/kg treated groups were 1.5 and 1.1.
Reduced inflammatory cell infiltrates, epithelial hyperplasia and mucin depletion from goblet cells in the colon at 0.3 mg/kg.
Animal Model: Immunodeficient SCID mice with chronic colitis induced by adoptive transfer of CD4+CD45RBhigh T cells from BALB/c mice[3].
Dosage: 0.1, 0.3 mg/kg
Administration: p.o., daily, 21 days, the anti-mTNF-α mAb (250 μg/mouse) was intraperitoneally injected on days 7 and 21.
Result: Increased body weight from day 15 comparable to anti-mTNF-α mAb-treated groups.
Clinical scores in the 0.1 and 0.3 mg/kg treated groups were 1.1 and 0.6 and anti-mTNF-α mAb-treated group was 1.2.
Inhibited the development of chronic colitis with an efficacy comparable to that of an anti-mTNF-α mAb (250 μg/mouse).
Animal Model: Immunodeficient SCID mice with chronic colitis induced by adoptive transfer of CD4+CD45RBhigh T cells from BALB/c mice[3].
Dosage: 0.3 mg/kg
Administration: p.o., daily, 3-4 weeks
Result: Significantly reduced the number of infiltrating lymphocytes and CD4+ T cells.
Decreased the number of IFN-γ- and IL-17-producing CD4+ T cells in the lamina propria.
Produced significantly less IFN-γ and IL-17 than those from vehicle-treated mice.
Animal Model: MRL/lpr mice at 8 weeks of age without proteinuria[4].
Dosage: 0.1, 0.3, 1 mg/kg
Administration: p.o., daily, 18 weeks
Result: No mice treated at doses greater than 0.3 mg/kg developed lupus nephritis during the study period.
Reduced this infiltration of T cells into the kidneys.
Inhibited the development of lymphadenopathy and splenomegaly.
Decreased the number of T cells,CD4 T cells, B cells, and MRL/lpr-mouse-specific abnormal T cells.
Animal Model: NZBWF1 mice at 30 weeks of age without proteinuria[4].
Dosage: 0.1, 0.3 mg/kg
Administration: p.o., daily, 10 weeks
Result: Mean proteinuria scores remained lower than those in the control group.
Attenuated the severity of several histological changes including mesangial expansion, glomerular sclerosis, and interstitial infiltrates.
Animal Model: NZBWF1 mice at 41 weeks of age without proteinuria[4].
Dosage: 0.3 mg/kg
Administration: p.o., daily, 13 weeks
Result: Reduced the number of infiltrating T cells, CD4 T cells, CD8 T cells, and CD4-CD8- double-negative (DN) T cells.
Decreased B cell counts.
Clinical Trial
分子量

377.44

Formula

C19H30F3NO3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Amiselimod 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Amiselimod942399-20-4MT-1303MT1303MT 1303LPL ReceptorLysophospholipid Receptororally activeS1P1bradycardia effectsS1P5S1P4autoimmune diseasesHCMshuman cardiac myocyteschronic colitislupus nephritisInhibitorinhibitorinhibit

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