country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-111193A

Copy Link Print Information

Declopramide hydrochloride

(別名: 3-Chloroprocainamide hydrochloride)

Declopramide (3-Chloroprocainamide) hydrochloride is an orally active, blood-brain barrier-permeable IκBβ/NF-κB inhibitor and chemosensitizer. Declopramide exhibits affinity for rabbit 5-HT₃ receptors (5-HT₃R) with a K_i value of 3.2 μM. Declopramide inhibits IκBβ degradation, blocks NFκB activation, and induces rapid apoptosis and DNA strand breaks in cancer cells. Declopramide enhances the cytotoxicity induced by Cisplatin (HY-17394) and is also metabolically converted to N-acetyl declopramide. Declopramide can be used in the research of tumors such as brain astrocytoma.

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: 52423-57-1
分子式: C₁₃H₂₁Cl₂N₃O
分子量:306.23

保管条件:

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

Declopramide hydrochloride 構造式

CAS 番号: 52423-57-1

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性

製品説明

体外実験

Declopramide (250-1000 µM; 20 h) hydrochloride induces dose-dependent caspase-mediated early apoptosis in 70Z/3 mouse pre-B cells^[1].
Declopramide (250-1000 µM; 24 h) hydrochloride inhibits LPS (HY-D1056)-induced activation of NF-κB in 70Z/3 mouse pre-B cells^[1].
Declopramide inhibits the growth of HL60 and K562 leukemia cells in vitro, but its activity is weaker than that of its metabolite N-acetyl-declopramide^[2].

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

Apoptosis Analysis^[1]

Cell Line:

murine pre-B-cell line 70Z/3
Concentration:

250 µM; 500 µM; 1000 µM; 500 µM (with 1 h ZVADfmk pretreatment)
Incubation Time:

20 h; 17 h (with 1 h ZVADfmk pretreatment)
Result:

Induced a dose-dependent increase in early apoptosis (Annexin V-positive/7AAD-negative cells) and corresponding decrease in viable (7AAD-negative) cells in 70Z/3 cells.
Reduced viable cell percentage and increased early apoptotic cell percentage relative to untreated cells at 500 µM.
Significantly reduced declopramide-induced apoptosis when caspase inhibitor ZVADfmk was used, measured via both 7AAD and Annexin V staining.

体内実験

Declopramide (40 mg/kg; p.o.; administered 3 times) hydrochloride exerts a significant inhibitory effect on tumor growth in SCID mice bearing human T24 brain astrocytoma xenografts^[2].
Declopramide (25-200 mg/kg; i.m., p.o.; single dose) hydrochloride does not induce central nervous system-related sedative side effects in female Wistar-Furth rats^[3].
Declopramide (25 mg/kg; i.m., p.o.; single dose) hydrochloride distributes to the brain, spleen and tumor tissues in scid mice bearing H2981 xenografts^[3].

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

Animal Model:

SCID mice (xenografted with human T24 brain astrocytoma cells)^[2]
Dosage:

40 mg/kg
Administration:

p.o.; 3 doses at 0, 24, and 48 hours
Result:

Exhibited equivalent in vivo tumor growth inhibitory efficacy to intramuscularly administered 40 mg/kg declopramide.

Animal Model:

Wistar-Furth (female, 2 months old, ~200 g)^[3]
Dosage:

25 mg/kg; 200 mg/kg
Administration:

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

Showed no observable sedative side effects or notable symptoms across all tested doses and observation periods.
Detected no significant differences in tunnel travel time between declopramide-treated rats and control rats at any dosage, administration route, or time point.

化学情報

CAS 番号 52423-57-1
分子量 306.23
分子式 C₁₃H₂₁Cl₂N₃O
SMILES

O=C(C1=CC=C(C(Cl)=C1)N)NCCN(CC)CC.Cl
別名

3-Chloroprocainamide hydrochloride
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.