| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Isoforskolin is a potent activator of adenylyl cyclase, increasing intracellular cAMP levels. It binds to the catalytic subunit of adenylyl cyclase, enhancing the conversion of ATP to cAMP. Elevated cAMP activates PKA, which then modulates multiple downstream pathways, including CREB, and inhibits NF-κB and MAPK, leading to anti-inflammatory and cardioprotective effects. It may also act on TRPV1 channels.
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| ln Vitro |
Recombinant Borrelia burgdorferi basic membrane protein A (rBmpA) induces the transcription and production of TNF-α and IL-6, which is downregulated by isoforskolin [1].
In vitro, isoforskolin stimulates cAMP production in various cell types with an EC50 of 1-5 µM, similar to forskolin but with slightly different selectivity. It inhibits LPS-induced NO and TNF-α production in macrophages with IC50 values of 2-5 µM. It shows moderate cytotoxicity against cancer cell lines (e.g., A549 IC50 ~ 20 µM) after 48 h. |
| ln Vivo |
In vivo, isoforskolin has shown cardioprotective effects in rat models of myocardial ischemia-reperfusion injury. Intravenous administration of 1-5 mg/kg reduced infarct size and improved cardiac function. It also lowers blood pressure in spontaneously hypertensive rats (5 mg/kg, i.p.). In a mouse model of asthma, isoforskolin (10 mg/kg, p.o.) reduced airway inflammation and hyperresponsiveness.
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| Enzyme Assay |
The in vitro adenylyl cyclase activity assay uses membrane fractions from rat brain or recombinant enzyme. Isoforskolin (0.01-100 µM) is incubated with ATP and the enzyme in buffer containing Mg²⁺ and GTP. cAMP produced is measured by ELISA or radioimmunoassay. The EC50 is determined. For anti-inflammatory assays, RAW 264.7 cells are treated with isoforskolin and stimulated with LPS, and cytokines are measured.
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| Cell Assay |
For in vitro cell-based assays, macrophage cell lines are seeded in 96-well plates and treated with isoforskolin (0.1-50 µM) for 2 h, then LPS (1 µg/mL) for 24 h. NO is measured by Griess, and TNF-α by ELISA. Intracellular cAMP is measured using a commercial kit. For cell viability, cancer cells are treated for 48 h and assessed by MTT.
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| Animal Protocol |
In vivo myocardial ischemia-reperfusion studies are performed in male Sprague-Dawley rats. Rats are anesthetized, and the left anterior descending coronary artery is ligated for 30 min, followed by reperfusion for 2 h. Isoforskolin is given intravenously at 0.5, 1, or 5 mg/kg before reperfusion. Infarct size is determined by TTC staining. Blood pressure is monitored via carotid artery catheter.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for isoforskolin are limited. In rats, after intravenous injection (1 mg/kg), the half-life is about 1.5 h, and volume of distribution is 2 L/kg. Oral bioavailability is low (<10%) due to first-pass metabolism. The compound is metabolized by CYP450 and excreted in bile. Plasma protein binding is ~80%.
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| Toxicity/Toxicokinetics |
In acute toxicity studies, the intravenous LD50 in mice is ~50 mg/kg. Oral administration is better tolerated (LD50 > 1000 mg/kg). At therapeutic doses (1-5 mg/kg), no significant adverse effects are observed. High doses may cause hypotension and tachycardia due to excessive cAMP elevation. No genotoxicity or organ toxicity is reported.
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| References | |
| Additional Infomation |
There have been reports of isothrixin being detected in the lacquer tree (Excoecaria cochinchinensis), and relevant data are available for reference.
Isoforskolin is a minor constituent of Coleus forskohlii. It has been studied as a potential cardioprotective and anti-inflammatory agent. Its mechanism is similar to forskolin but with distinct pharmacokinetics. No clinical trials have been conducted. It is used as a research tool for studying cAMP signaling. |
| Molecular Formula |
C22H34O7
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|---|---|
| Molecular Weight |
410.5012
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| Exact Mass |
410.23
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| CAS # |
64657-21-2
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| PubChem CID |
9549169
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
524.5±50.0 °C at 760 mmHg
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| Flash Point |
173.6±23.6 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.552
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
747
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC(=O)O[C@H]1[C@@H]2[C@]([C@H](CCC2(C)C)O)([C@]3(C(=O)C[C@](O[C@@]3([C@H]1O)C)(C)C=C)O)C
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| InChi Key |
CLOQVZCSBYBUPB-KGGHGJDLSA-N
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| InChi Code |
InChI=1S/C22H34O7/c1-8-19(5)11-14(25)22(27)20(6)13(24)9-10-18(3,4)16(20)15(28-12(2)23)17(26)21(22,7)29-19/h8,13,15-17,24,26-27H,1,9-11H2,2-7H3/t13-,15-,16-,17-,19-,20-,21+,22-/m0/s1
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| Chemical Name |
[(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-5,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-5,6,6a,8,9,10-hexahydro-2H-benzo[f]chromen-6-yl] acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 1.2180 mL | 2.4361 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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