Bucladesine (Dibutyryl cAMP; DBcAMP) sodium (GMP) is a Bucladesine sodium (HY-B0764) produced by using GMP guidelines. Bucladesine (Dibutyryl cAMP; DBcAMP) is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation.
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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: 16980-89-5
- 分子式: C18H23N5NaO8P
- 分子量:491.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
28.9 μM
Compound: dbcAMP
|
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA
|
[PMID: 11000020] |
| Vero C1008 | IC50 |
>2.0 × 105M
Compound: COVC-3360888908
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
10.6019/CHEMBL4651402 |
Bucladesine causes significant growth delay in multicellular tumor spheroids derived directly from human malignant brain tumors[1].
Bucladesine augments differentiation therapy (in combination with Sodium butyrate (HY-B0350A) and hyperthermia) in human and canine brain tumor cells in vitro[1].
Bucladesine suppresses the mitogenic effects of platelet-derived growth factor (PDGF), basic fibroblast growth factor (bFGF), and epidermal growth factor (EGF) on human astrocytoma cells; bucladesine alone neither potentiates nor inhibits human astrocytoma cell growth[1].
Bucladesine suppresses proliferation, enhances cytoplasmic process formation, increases cytoplasmic glial fibrillary acidic protein (GFAP) levels, and suppresses malignant glioma invasion by decreasing CD44 isoform expression in cultured malignant glioma cells, inducing biochemical and morphological changes[1].
Bucladesine decreases Bcl-2 levels and enhances SNAP-induced p53-sensitive cell death and MPP+-induced cell death, sensitizing human neuroblastoma cells to apoptosis[1].
Bucladesine inhibits proliferation and induces morphological differentiation of astrocytes in vitro via a cyclic adenosine monophosphate-dependent protein kinase pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Bucladesine (50-300 nM/mouse; i.p.; single dose) exerts a biphasic anti-nociceptive effect on thermal-induced acute pain in male albino mice, with significant activity at 50 and 100 nM/mouse doses, no significant effect at 300 nM/mouse[3].
Bucladesine (0.5-1.5% cream, 5% solution; topical; single or two doses) produces a statistically significant reduction in Arachidonic acid (HY-109590)-induced acute skin inflammation in Mus musculus, with single administration of 1.5% cream yielding a 28% reduction in ear swelling and two administrations yielding a 24% reduction[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 16980-89-5
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分子量 491.37
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分子式 C18H23N5NaO8P
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SMILES
O=C(CCC)O[C@H]1[C@H](N2C(N=CN=C3NC(CCC)=O)=C3N=C2)O[C@@](CO4)([H])[C@@]1([H])OP4(O[Na])=O
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別名
Dibutyryl cAMP sodium (GMP); DBcAMP sodium (GMP)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
参考文献
[1]. Dalbasti T, et al. Local interstitial chemotherapy with sustained release bucladesine in de novo glioblastoma multiforme: a preliminary study. J Neurooncol. 2002;56(2):167-174. [Content Brief]
[2]. Taghizadeh G, et al. Bucladesine Attenuates Spatial Learning and Hippocampal Mitochondrial Impairments Induced by 3, 4-Methylenedioxymethamphetamine (MDMA). Neurotox Res. 2020;38(1):38-49. [Content Brief]
[3]. Salehi F, et al. Effect of bucladesine, pentoxifylline, and H-89 as cyclic adenosine monophosphate analog, phosphodiesterase, and protein kinase A inhibitor on acute pain. Fundam Clin Pharmacol. 2017;31(4):411-419. [Content Brief]
[4]. Rundfeldt C, et al. The stable cyclic adenosine monophosphate analogue, dibutyryl cyclo-adenosine monophosphate (bucladesine), is active in a model of acute skin inflammation. Arch Dermatol Res. 2012;304(4):313-317. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)