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製品番号: HY-119247

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NBI 30545

NBI 30545 is a blood-brain barrier permeable CRF1R antagonist with a K_i value of 3.4 nM for the human receptor. NBI 30545 inhibits CRF-stimulated intracellular cAMP accumulation and ACTH release. NBI 30545 can be used in the research of depression, anxiety disorders and stress-related diseases.

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。

CAS 番号: 195054-99-0
分子式: C₂₂H₃₀N₄O₃
分子量:398.51

保管条件:

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

NBI 30545 構造式

CAS 番号: 195054-99-0

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価格（税別）

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数量

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Fluorescent Dye

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

生物活性
- 製品説明
- Cellular Effect
- 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

CRFR アイソフォーム固有の製品をすべて表示 :

CRFR1
CRFR2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	76 nM Compound: 8	Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor	[PMID: 15341493]
Pituitary gland cell	IC₅₀	37 nM Compound: 18n	Inhibition of CRF-stimulated ACTH release in cultured rat anterior pituitary cells Inhibition of CRF-stimulated ACTH release in cultured rat anterior pituitary cells	[PMID: 15203140]
Pituitary gland cell	IC₅₀	76 nM Compound: 18n	Inhibition of CRF-stimulated cAMP production in cultured rat anterior pituitary cells Inhibition of CRF-stimulated cAMP production in cultured rat anterior pituitary cells	[PMID: 15203140]

体外実験

NBI 30545 inhibits CRF-stimulated cAMP accumulation in cells expressing the human CRF₁ receptor with an IC₅₀ of 76 nM^[1].
NBI 30545 inhibits CRF-stimulated ACTH release in cultured rat anterior pituitary cells with an IC₅₀ of 37 nM^[1].

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

Parmacokinetics

Species	Dose	Route	V_d	CL	T_1/2	AUC	Brain-Kp (AUC_last)	Bioavailability
Rat^[1]	10 mg/kg	i.v.	4.7 L/kg	43 mL/min/kg	1.1 h	/	/	/
Rat^[1]	10 mg/kg	p.o.	/	/	/	1182 ng·h/mL	1472 ng/g·h	30.5 %

体内実験

NBI 30545 (Compound 18n) (10 mg/kg; i.v., p.o.; single dose) achieves good oral plasma and brain exposure in rats with a 30.5% bioavailability and 1.2 brain/plasma ratio, along with extensive tissue distribution and a short half-life after intravenous administration^[1].

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

Animal Model:

Sprague-Dawley^[1]
Dosage:

10 mg/kg (i.v.); 10 mg/kg (p.o.)
Administration:

i.v.; single dose; p.o.; single dose
Result:

Achieved a volume of distribution of 4.7 L/kg, clearance of 43 mL/min/kg, and a half-life of 1.1 h after intravenous administration.
Reached a plasma AUC of 1182 ng/mL·h, brain AUC of 1472 ng/g·h, oral bioavailability of 30.5%, and a brain/plasma ratio of 1.2 after oral administration.

化学情報

CAS 番号 195054-99-0
分子量 398.51
分子式 C₂₂H₃₀N₄O₃
SMILES

N1=C(C=C(N2N=C(C(=C12)C=3C=CC(OC)=CC3OC)C)N(CCOC)CCC)C
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

取扱説明書 (2659 KB)

参考文献

[1]. Chen C, et al. Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility. Bioorg Med Chem Lett. 2004;14(14):3669-3673. [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.

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MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- 体外実験
- 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

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NBI 30545

CRFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

NBI 30545 関連分類

HY-119247 関連分類