>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>Forskolin

Forskolin (Synonyms: Coleonol, HL 362, L 751362B, NSC 357088, NSC 375489)

Catalog No.GC11920

Forskolin은 type I adenylyl cyclase를 41nM의 IC50로 가지는 강력한 adenylyl cyclase 활성화제이다.

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Forskolin Chemical Structure

Cas No.: 66575-29-9

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$42.00
재고 있음
25mg
US$53.00
재고 있음
50mg
US$73.00
재고 있음
100mg
US$115.00
재고 있음
2g
US$390.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 5 publications

Description of Forskolin

Forskolin은 type I adenylyl cyclase를 41nM의 IC50로 가지는 강력한 adenylyl cyclase 활성화제이다.

Forskolin은 EC50가 0.5 μM로, 세포 내 cAMP 형성을 촉진하는 인도체이기도 한다. Forskolin은 다양한 세포의 분화를 유도하고, 프로게스터온 X 수용체(PXR)와 FXR를 활성화한다. Forskolin은 심장에 수축 작용을 미치며, 혈소판 응집 억제 및 혈압 감소 효과가 있다. Forskolin은 또한 autophagy를 유도한다.

Forskolin (Coleonol)은 전립선 암 세포에서 강력한 exosome biogenesis 및/또는 비밀 활성화제이기도 한다. Forskolin은 인간 적혈구 셀막의 자유질자 스트레스를 조절하고 심혈관질환과 당뇨병 치료의 전망을 제공한다. Forskolin으로 인한 cAMP 증가는 세포 독성과 세포사를 완화시켰다.

인체 내 연구에서 포르스콜린은 건강한 쥐의 기초 포도당 수치를 주로 낮추고 당뇨병 쥐의 고혈당의 심각도를 완화시켰다. Mrp4(-/-) 쥐는 망막 혈관의 발달에서 명확한 이상을 보이지 않았지만, Mrp4(-/-) 쥐의 망막 혈관 발달은 Forskolin 투여에 반응하여 억제되었다. Forskolin 처리된 Mrp4(-/-) 쥐는 Ki67-positive와 cleaved caspase 3-positive ECs의 수가 증가하고, 주세포 pericyte coverage의 양이 현저하게 감소하고, empty sleeve의 수가 줄었다.

References:
[1]: Robbins JD, Boring DL, et,al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52. doi: 10.1021/jm960191+. PMID: 8709105.
[2]: Matsumiya W, Kusuhara S, et,al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35. doi: 10.1167/iovs.12-10781. PMID: 23154460; PMCID: PMC3517270.
[3]: Mayati A, Moreau A, et,al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115. doi: 10.1038/s41598-018-34421-8. PMID: 30382126; PMCID: PMC6208432.
[4]: Awad JA, Johnson RA, et,al. Interactions of forskolin and adenylate cyclase. Effects on substrate kinetics and protection against inactivation by heat and N-ethylmaleimide. J Biol Chem. 1983 Mar 10;258(5):2960-5. PMID: 6681815.
[5]: Seamon KB, Daly JW, et,al. Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J Med Chem. 1983 Mar;26(3):436-9. doi: 10.1021/jm00357a021. PMID: 6681845.
[6]: Ríos-Silva M, Trujillo X, et,al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11(5):448-52. doi: 10.7150/ijms.8034. PMID: 24688307; PMCID: PMC3970096.
[7]: Datta A, Kim H, et,al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. doi: 10.1038/s41598-018-26411-7. PMID: 29802284; PMCID: PMC5970137.
[8]:Niaz MA, Singh RB. Modulation of free radical stress in human red blood cell membrane by forskolin and the prospects for treatment of cardiovascular disease and diabetes. Cell Mol Biol (Noisy-le-grand). 1999 Dec;45(8):1203-7. PMID: 10643969.

Protocol of Forskolin

세포 실험 [1]:

세포 라인

PC 세포

제조 방법

세포는 엑소좀이 없는 FBS 보충 매체에서 Forskolin으로 처리되었으며 지정된 시간에 수확하여 후속 분석을 위해 사용하였습니다.

반응 조건

10 uM Forskolin, 72 시간 동안

응용 분야

Forskolin은 전립선암 세포 엑소좀이 생합성 및/또는 분비를 촉진하는 강력한 활성제입니다.
동물 실험 [2]:

동물 모형

10-14주령의 수컷 윌스타쥐, 평균 체중은 300g ± 50g입니다.

제조 방법

Forskolin (10mg캡슐)은 8주간 캐더를 통하여 구강으로 투여되었습니다. 매일 6mg/kg의 투여량은 인간의 1mg/kg일당과 동등합니다. Forskolin은 순수한 물에 희석되어 60mg/100의 농도로 되었습니다.

제형

매일 6mg/kg의 Forskolin, 8주간.

응용 분야

Forskolin은 건강한 쥐의 기초 포도당수치를 주로 낮추고 당뇨병 쥐의 고혈당의 심각도를 완화시켰습니다.

참고문헌:

[1]. Datta A, Kim H,et,al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. doi: 10.1038/s41598-018-26411-7. PMID: 29802284; PMCID: PMC5970137.

[2]. Ríos-Silva M, Trujillo X, et,al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11(5):448-52. doi: 10.7150/ijms.8034. PMID: 24688307; PMCID: PMC3970096.

Chemical Properties of Forskolin

Cas No. 66575-29-9 SDF
Synonyms Coleonol, HL 362, L 751362B, NSC 357088, NSC 375489
Chemical Name [(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-5,6,6a,8,9,10-hexahydro-2H-benzo[f]chromen-5-yl] acetate
Canonical SMILES CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O
Formula C22H34O7 M.Wt 410.5
Solubility ≥ 20.525mg/mL in DMSO Storage -20°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Forskolin

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.4361 mL 12.1803 mL 24.3605 mL
5 mM 0.4872 mL 2.4361 mL 4.8721 mL
10 mM 0.2436 mL 1.218 mL 2.4361 mL
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Related Video of Forskolin

    Forskolin-GlpBio

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Review for Forskolin

Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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