2. Membrane Transporter/Ion Channel
  3. Amino acid Transporter
  4. SLC6A19-IN-4

SLC6A19-IN-4 是一种变构竞争性且具有口服活性的 B0AT1 (SLC6A19) 抑制剂。SLC6A19-IN-4 对人和小鼠的 B0AT1 均具有抑制活性，IC50 值分别为 513 nM 和 295 nM。SLC6A19-IN-4 表现出优异的代谢稳定性。SLC6A19-IN-4 通过对肠道 (减少吸收) 和肾脏 (促进排泄) 中B0AT1 的双重抑制，能显著增加尿液中苯丙氨酸 (Phe) 的排泄并降低血浆 Phe 水平。 SLC6A19-IN-4 可用于苯丙酮尿症 (PKU) 及其他涉及 SLC6 家族转运蛋白疾病的研究。

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SLC6A19-IN-4

SLC6A19-IN-4 Chemical Structure

CAS No. : 2962069-39-0

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SLC6A19-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SLC6A19-IN-4 is an allosteric-competitive and orally active B⁰AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouse B⁰AT1b> with IC50 values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B⁰AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research[1].

体外研究
(In Vitro)

SLC6A19-IN-4 (1500-4000 nM) 在表达人源 SLC6A19 和人源 Collectrin 的 Jump-In TI platform 细胞中，增加了对 d5-Phe 摄取的 Km 值而不影响 Vmax 值，表明了其竞争性抑制特性 (Km 值分别为 0.866、5.19、12.1 mM；Vmax 值分别为 337、351、380 μmol/min/mg-protein)[1]。
SLC6A19-IN-4 在模拟细胞与小鼠 B⁰AT1 和 ACE2 共表达细胞中 Kd 为 123.1 nM，在模拟细胞与人源 B⁰AT1 和 ACE2 共表达细胞中的 Kd 为 46.98 nM[1]。

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

SLC6A19-IN-4 相关抗体:
体内研究
(In Vivo)

SLC6A19-IN-4 (30 mg/kg，口服，单次给药) 可通过减少肠道苯丙氨酸 (Phe) 吸收、促进尿液排泄，从而降低携带 F263S 纯合突变的雄性 Pahenu2 小鼠的全身 Phe 水平[1]。

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

Animal Model: Male Pahenu2 mice (12 weeks) carry a homozygous F263[1]
Dosage: 30 mg/kg
Administration: p.o., once
Result: Had a plasma concentration of 915 ng/ml and 1590 ng/ml at 4 and 8 hours post-dose.
Showed low membrane permeability 24.2 × 10-7 cm/s.
Increased urinary Phe excretion and concomitantly reduced plasma Phe concentrations 4 hours after dosing.
分子量

355.31

Formula

C16H16F3N3O3
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

SLC6A19-IN-4 相关分类

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Keywords:

SLC6A19-IN-42962069-39-0Amino acid Transporter氨基酸转运蛋白B?AT1orally activeintestinekidneyphenylketonuriaSLC6-familyInhibitorinhibitorinhibit

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