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FITM 纯度: 98.19%
FITM是mGlu1受体的负变构调节剂,Ki值为2.5 nM。
FITM Chemical Structure
CAS No. : 932737-65-0
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥740 | In-stock | |
2 mg | ¥500 | In-stock | |
5 mg | ¥900 | In-stock | |
10 mg | ¥1500 | In-stock | |
25 mg | ¥3000 | In-stock | |
50 mg | ¥5000 | In-stock | |
100 mg | ¥8500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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生物活性 |
FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
FITM fits tightly into the long and narrow pocket. Most of the ligand-receptor interactions are hydrophobic with the exception of the contacts of the pyrimidine-amine group with the T815 7.38 side chain. The mGlu1 binding pocket for FITM largely corresponds to mutagenic data for the common allosteric site in mGlus and likely extends to other class C GPCRs. FITM which shows high affinity and selectivity for mGlu1 over mGlu5[1]. FITM has the high hydrogen bonds occupancy with Thr815 and Tyr805 in dimer A and B of mGlu1 during molecular dynamics simulations. The nitrogen and hydrogen atoms of FITM form the dynamical hydrogen bonds with the hydrogen atom of Tyr805 and oxygen atom of Thr815, respectively. It indicates that there is a strong attraction interaction between FITM and allosteric sites[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
The pretreatment of rats with unlabeled FITM (1 mg/kg) occupies an mGluR1 binding site of 18F-FITM by more than 99% and does not affect the input function. The Kd (nM) and Bmax (pmol/mL) obtained by the Scatchard analyses with the multidose ligand assays are 2.1 and 36.3, respectively, for the thalamus; 2.1 and 27.5, respectively, for the hippocampus; 1.5 and 22.2, respectively, for the striatum; and 1.5 and 20.5, respectively, for the cingulate cortex with a high confidence[3]. 18F-FITM shows excellent pharmacokinetics, namely the dense and specific accumulation in mGlu1-positive melanomas versus mGlu1-negative hepatoma and normal tissues. Furthermore, the accumulation levels of radioactivity corresponded to the extent of tumor and to levels of mGlu1 protein expression in melanomas and melanoma metastasis[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
371.43 |
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Formula |
C18H18FN5OS |
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CAS 号 |
932737-65-0 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 150 mg/mL (403.84 mM) * “≥” means soluble, but saturation unknown. 配制储备液
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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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Animal Administration [3] |
Rats: Sprague–Dawley rats are treated with different doses of unlabeled FITM (0, 1, 5, or 30 μg/kg or 1 mg/kg) just before a bolus injection of 18F-FITM (17–18 MBq, 30–40 pmol, 0.1 mL). Estimations of equilibrium state and BPND were acquired[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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