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United States

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製品番号: HY-181753

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INSP-0154

INSP-0154 is a potent creatine kinase B (CKB)/creatine transporter (SLC6A8) inhibitor. INSP-0154 binds to the SLC6A8 occluded pocket, prevents creatine transport into cells, and protects SLC6A8 cysteine residue C144 from irreversible inactivation. INSP-0154 inhibits creatine uptake in mouse heart tissue. INSP-0154 can be used for the research of cancer.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₆H₁₀N₄O₂
分子量:170.17

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

INSP-0154 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

SLC6A8

体外実験

INSP-0154 (Compound 46) (0.46-1000 μM; 1 h) potently inhibits SLC6A8-mediated creatine uptake in HCT-116 cells with an IC₅₀ of 8.2 μM^[1].
INSP-0154 (0.46-1000 μM) inhibits GAT-2, GAT-3, BGT-1, and TAUT-mediated creatine uptake with IC₅₀ of 22.7, 150, 116 and 11.9 μM, while showing no activity against GAT-1 at concentrations up to 1000 μM^[1].
INSP-0154 shows strong in vitro plasma and metabolic stability, low Caco-2 permeability, and is not a P-gp efflux substrate^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_last	T_1/2	F	C₀
Mice^[1]	3 mg/kg	i.v.	/	/	2151 ng·h/mL	0.9 h	/	7698 ng/mL
Mice^[1]	100 mg/kg	p.o.	13517 ng/mL	0.5 h	30616 ng·h/mL	2.7 h	42.7 %	/
Mice^[1]	100 mg/kg	i.p.	42700 ng/mL	0.5 h	27742 ng·h/mL	3.3 h	59.6 %	/

体内実験

INSP-0154 (Compound 46) (100 mg/kg; i.p.; single dose) inhibits creatine transport in mouse heart tissue^[1].

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

Animal Model:

C57BL/6 (male, 6−9 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

i.p.; single dose
Result:

Achieved inhibition of creatine-d₃ uptake in heart tissue, with greater potency than β-GPA under the tested conditions.

化学情報

分子量 170.17
分子式 C₆H₁₀N₄O₂
SMILES

[H][C@]12CN(C[C@]1(C(NO2)=O)[H])C(N)=N
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Martinez EJ, et al. Carboxylic Acid Bioisosteres of Creatine as Novel and Selective Substrate Competitive Inhibitors of the Creatine Transporter SLC6A8. J Med Chem. 2026;69(4):3915-3931. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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