Home Cart Sign in  
Chemical Structure| 66575-29-9 Chemical Structure| 66575-29-9

Structure of Forskolin
CAS No.: 66575-29-9

Chemical Structure| 66575-29-9

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Forskolin is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types with binding (IC50=41 nM) to and activation (EC50=0.5 μM) of type I adenylyl cyclase. It is commonly used to raise levels of cAMP in the research of cell physiology.

Synonyms: Coleonol; Colforsin; NSC 375489

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

DE Stock

US Stock

Asia Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Product Citations

Aldrich, Jane V ; Yakovlev, Dmitry Y ; Coleman, Jeremy S ; Senadheera, Sanjeewa N ; Stacy, Heather M ; Eans, Shainnel O , et al.

Abstract: Kappa opioid receptor (KOR) antagonists may have therapeutic potential to prevent stress-induced relapse in abstinent individuals with cocaine use disorder (CUD). The macrocyclic peptide [D-Trp]CJ-15,208 (cyclo[Phe-D-Pro-Phe-D-Trp]) is an orally bioavailable, brain–penetrant selective KOR antagonist that prevents stress-induced reinstatement of cocaine-seeking behavior in a mouse model of CUD. We synthesized and evaluated analogs of this lead compound with substitutions for the D-Trp residue to identify analogs that exhibit more potent central KOR antagonism following oral administration. The peptides were synthesized by a combination of solid phase and solution peptide synthetic methodologies, and their pharmacological activity was evaluated both in vitro (for KOR affinity, selectivity and antagonism) and in vivo (for antinociception and KOR antagonism), with promising analogs evaluated for their ability to prevent stress-induced reinstatement of cocaine-seeking behavior in the mouse conditioned place preference (CPP) assay. A variety of substituted D-Phe or modified D-Trp derivatives were tolerated by KOR with retention of significant KOR antagonism in vivo after oral administration. Macrocyclic peptide pretreatment, per os, significantly prevented stress-induced reinstatement of cocaine CPP at doses of 10 and 30 mg/kg of [D-Phe4]CJ-15,208, 4, and 30 mg/kg of [D-Trp(formamide)]CJ-15,208, 3, which are 6-fold and 2-fold lower, respectively, than that needed for {D-Trp]CJ-15,208.

Keywords: [D-Trp]CJ-15,208 ; kappa opioid receptor antagonist ; brain-penetrant peptides ; orally active peptides ; cocaine abuse ; stress-induced reinstatement

Purchased from AmBeed:

Alternative Products

Product Details of Forskolin

CAS No. :66575-29-9
Formula : C22H34O7
M.W : 410.50
SMILES Code : CC(=O)O[C@H]1[C@H]([C@@H]2[C@]([C@H](CCC2(C)C)O)([C@@]3([C@@]1(O[C@@](CC3=O)(C)C=C)C)O)C)O
Synonyms :
Coleonol; Colforsin; NSC 375489
MDL No. :MFCD00082317
InChI Key :OHCQJHSOBUTRHG-KGGHGJDLSA-N
Pubchem ID :47936

Safety of Forskolin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H312
Precautionary Statements:P280

Related Pathways of Forskolin

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293A cells 1–10 μM 1 h To assess the inhibitory effect of Forskolin on mTORC1 activity Elife. 2019 May 21;8:e43038.
MEF cells 10 μM 1 h To assess the inhibitory effect of Forskolin on mTORC1 activity Elife. 2019 May 21;8:e43038.
HEK293T cells 30 μM 30 min Enhanced the interaction between DAGLα and ankyrin-G Biol Psychiatry. 2021 Aug 15;90(4):263-274.
GLUTag cells 10 μM 15 min and 30 min Measure cAMP concentration and PKA activity Gut Microbes. 2021 Jan-Dec;13(1):1987782.
WT cells 10 µM 48 h To investigate the effect of Forskolin on cell respiration and ATP synthesis, results showed that Forskolin increased cell respiration and ATP synthesis. EMBO Mol Med. 2009 Nov;1(8-9):392-406.
CHO-K1 cells 20 µM 30 min Activate PKA to study its effect on KCTD12-induced K+ current desensitization. Results showed that PKA activation significantly slowed KCTD12-induced fast desensitization. Biochem Pharmacol. 2014 Oct 1;91(3):369-79.
Hippocampal neurons 20 µM 30 min Activate PKA to study its effect on KCTD12-induced K+ current desensitization. Results showed that PKA activation significantly slowed KCTD12-induced fast desensitization. Biochem Pharmacol. 2014 Oct 1;91(3):369-79.
MIN6 cells 10 μM 30 min To assess cAMP production, results showed that forskolin-stimulated cAMP production was significantly reduced in Npas4-overexpressing MIN6 cells Diabetes. 2013 Aug;62(8):2808-20.
ScN2a-cl3 cells 1 μM 7 days To evaluate the effect of Forskolin on PrPSc levels in differentiated cells. Results showed that Forskolin did not lead to a rebound in PrPSc levels. PLoS Pathog. 2009 Nov;5(11):e1000673.
Primary cortical neurons 30 μM 30 min Increased the interaction between DAGLα and ankyrin-G and regulated dendritic spine morphology Biol Psychiatry. 2021 Aug 15;90(4):263-274.
SKOV3 cells 20 μM 30 to 40 min Induced endogenous EPAC1 nuclear oligomer formation Nat Commun. 2023 Sep 8;14(1):5521
HUVEC cells 20 μM 30 to 40 min Induced endogenous EPAC1 nuclear oligomer formation Nat Commun. 2023 Sep 8;14(1):5521
HEK cells 20 μM 30 to 40 min Induced EPAC1-YFP nuclear oligomer formation Nat Commun. 2023 Sep 8;14(1):5521

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice PSNL and CFA models Oral 2 mg/kg Once daily for 14–33 days Forskolin reversed the PSNL- or CFA-induced decrease in PKA and CREB phosphorylation and BDNF expression, and partially reversed mechanical hypersensitivity and depression-like behaviors Int J Neuropsychopharmacol. 2024 Oct 1;27(10):pyae040
Mice Not specified Intraperitoneal injection 1 mg/kg Single dose, lasting 30 minutes Enhance endothelial cell barrier function, reduce permeability and immune complex deposition J Exp Med. 2004 Oct 4;200(7):835-46
Mice WT and AnkG cKO mice Intraperitoneal injection 0.2 mg/kg Single injection, behavioral tests conducted 30 minutes after injection Evaluated the effect of forskolin on depression- and anxiety-related behaviors, finding that forskolin could not reverse depression-related behavior in AnkG cKO mice but could reverse anxiety-related behavior Biol Psychiatry. 2021 Aug 15;90(4):263-274.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03390985 - Completed - -
NCT02586883 Idiopathic Dilation of the Bro... More >>nchi Less << Not Applicable Recruiting April 2020 France ... More >> Necker-Enfants Malades Hospital Recruiting Paris, France, 75015 Contact: Isabelle SERMET-GAUDELUS, MD, PhD    +33144494887    isabelle.sermet@nck.aphp.fr Less <<
NCT03455153 - Completed - United Kingdom ... More >> Lindum Medical Practice Lincoln, Lincolnshire, United Kingdom, LN2 2JP Nettleham Medical Practice Lincoln, Lincolnshire, United Kingdom, LN2 2RS Birchwood Medical Practice Lincoln, Lincolnshire, United Kingdom, LN6 0QQ Less <<
NCT01920841 Weight Loss Not Applicable Withdrawn(Study Design changed... More >> and will be resubmitted as a new study) Less << - United States, Louisiana ... More >> Pennington Biomedical Research Center Baton Rouge, Louisiana, United States, 70808 Less <<
NCT03652090 - Completed - -
NCT02143349 Metabolic Syndrome ... More >> Obesity Less << Phase 3 Unknown May 2015 Australia, Victoria ... More >> College of Health and Biomedicine Victoria University Recruiting St. Albans, Victoria, Australia, 14428 Contact: Dr. Xiao Su    +61399192318    xiao.su@vu.edu.au    Contact: A/Prof Michael Mathai    +61399192211    michael.mathai@vu.edu.au    Principal Investigator: Dr. Xiao Su          Sub-Investigator: A/Prof Michael Mathai Less <<
NCT00864578 - Withdrawn(loss of interest bef... More >>ore enrolment started) Less << June 2009 Italy ... More >> Ophthalmology Department of the University Clinic Bari, Italy, I-70124 Less <<
NCT02807415 - Recruiting June 2019 Germany ... More >> Justus-Liebig-University Recruiting Gießen, Germany, 35385 Contact: Lutz Nährlich, MD    004964198557620    lutz.naehrlich@paediat.med.uni-giessen.de    Contact: Claudia Rückes-Nilges, Dipl-Biol    004964198556945    claudia.rueckes-nilges@paediat.med.uni-giessen.de    Principal Investigator: Lutz Nährlich, MD          Sub-Investigator: Stefan Kuhnert, MD          Hannover Medical School Recruiting Hannover, Germany, 30625 Contact: Burkhard Tümmler, MD PhD    00495115322920    tuemmler.burkhard@mh-hannover.de    Contact: Christian Dopfer, MD    00495115326111    dopfer.christian@mh-hannover.de    Principal Investigator: Burkhard Tümmler, MD PhD          Sub-Investigator: Christian Dopfer, MD          University of Heidelberg Recruiting Heidelberg, Germany, 69120 Contact: Marcus Mall, MD    00496221564502    Marcus.Mall@med.uni-heidelberg.de    Contact: Simon Gräber, MD    004962215638926    Simon.Graeber@med.uni-heidelberg.de    Principal Investigator: Marcus Mall, MD          Sub-Investigator: Simon Gräber, MD          Sub-Investigator: Susanne Dittrich, MD Less <<
NCT00863811 - Withdrawn(loss of interest bef... More >>ore enrolment started) Less << July 2009 Italy ... More >> Ophthalmology Department of the University Bari, Italy, I-70124 Less <<
NCT01254006 Glaucoma Not Applicable Completed - Italy ... More >> Univerisity La Sapienza Latina, Italy Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.18mL

2.44mL

1.22mL

24.36mL

4.87mL

2.44mL

References

 

Historical Records

Categories