| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SSTR1 2.8 nM (IC50) SSTR2 7.1 nM (IC50) SSTR3 0.2 nM (IC50) SSTR4 3.0 nM (IC50) SSTR5 13.7 nM (IC50)
Cortistatin 29 binds with high affinity to all five human somatostatin receptor (SSTR) subtypes (SSTR1-5). It exhibits IC50 values of 2.8 nM for SSTR1, 7.1 nM for SSTR2, 0.2 nM for SSTR3, 3.0 nM for SSTR4, and 13.7 nM for SSTR5. It also inhibits cAMP production induced by forskolin through SSTRs. |
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| ln Vitro |
Cortistatin 29 shows in vitro activity through binding to SSTR subtypes. It inhibits forskolin-induced cAMP accumulation in cells expressing SSTRs. The potency for cAMP inhibition correlates with its receptor binding affinity, with highest potency at SSTR3 (IC50 0.2 nM). It is found at similar levels as cortistatin-14 in mouse AtT20 cells but is secreted at a lower level.
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| ln Vivo |
In mice, cortistatin 29 (1-2 µg) reduces chronic neuropathic pain[1]. Mouse studies have demonstrated the anti-fibrotic properties of cortistatin 29 (1 nmol/mouse; ip; three times weekly)[4].
In vivo, Cortistatin 29 (1-2 microg per mouse) alleviates chronic neuropathic pain in mouse models. It also shows anti-fibrotic effects at a dose of 1 nmol/mouse administered via intraperitoneal (i.p.) injection three times weekly. It has demonstrated efficacy in reducing pain-related behaviors and fibrotic tissue formation. |
| Enzyme Assay |
Cortistatin 29 is evaluated using standard radioligand binding assays for somatostatin receptors. Membranes from CHO-K1 cells stably expressing human SSTR1-5 are incubated with 0.05 nM [125I]Tyr11-somatostatin-14 in binding buffer. Varying concentrations of Cortistatin 29 (0-1000 nM) are added. Non-specific binding is determined with 1 microM somatostatin-14. After 60 minutes at 25degC, bound radioactivity is measured by filtration. IC50 values are calculated.
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| Cell Assay |
For cell-based assays, CHO-K1 cells stably expressing human SSTR1-5 are seeded in 96-well plates (25,000 cells/well). Cells are pre-incubated with 500 microM IBMX (phosphodiesterase inhibitor) for 10 minutes at 37degC. Cortistatin 29 (0-1000 nM) is added, followed by 1 microM forskolin (to stimulate cAMP). After 30 minutes at 37degC, cAMP accumulation is measured using an HTRF or chemiluminescence-based cAMP immunoassay. EC50 values are calculated from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: 20-24 g body weight, 8-12 weeks-old mice[1]
Doses: 1 µg in 20 µL for sc; 2 µg in 200 µL for ip; 20 ng in 10 µL for it Route of Administration: Every other day for 12 days Experimental Results: Ameliorated hyperalgesia and allodynia, regulated the nerve damageinduced hypersensitization of primary nociceptors, inhibited neuroinflammatory responses, and enhanced the production of neurotrophic factors both at the peripheral and central levels. Animal/Disease Models: 20-24g body weight, 8-10 weeks-old C57BL/6 mice (CST+/+, CST+/- and CST-/- mice)[4]. Doses: 1 nmol/mouse Route of Administration: Ip, three times weekly from 5 or 14 days Experimental Results: Reversed in vivo and in vitro these exaggerated fibrogenic phenotypes and Protected from progression to severe liver fibrosis in response to hepatic injury. For in vivo animal studies, chronic neuropathic pain is induced in male C57BL/6 mice (6-8 weeks) using the spared nerve injury (SNI) model or chronic constriction injury (CCI). Cortistatin 29 is dissolved in saline and administered via intraperitoneal injection (1-2 microg per mouse) on post-operative days 7, 10, and 14. Mechanical allodynia and thermal hyperalgesia are assessed using von Frey filaments and the Hargreaves test. For anti-fibrosis studies, mice receive Cortistatin 29 (1 nmol/mouse; i.p.) three times weekly for 3-4 weeks. Tissues are collected for histological analysis (Masson's trichrome staining) and fibrosis marker measurement (hydroxyproline, alpha-SMA, collagen I). |
| ADME/Pharmacokinetics |
Cortistatin 29 is a 29-amino acid peptide with molecular formula C159H244N44O44S4 (monoisotopic MW approximately 3615.2 Da). It is supplied as a lyophilized powder (typically as TFA salt). It is soluble in water and DMSO (e.g., 1 mg/mL in water). It is stored at -20degC, protected from light and moisture. Reconstituted solutions are stable for short periods at 4degC but repeated freeze-thaw cycles should be avoided.
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| Toxicity/Toxicokinetics |
Cortistatin 29 is a research-grade peptide not for human use. At the research doses described (1-2 microg per mouse), no significant toxicity has been reported. Standard safety precautions for handling peptides (avoid inhalation, skin contact) should be followed. Purity is typically ≥95-98% by HPLC. It is for laboratory research purposes only.
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| References |
[1]. Falo CP, et al. The Neuropeptide Cortistatin Alleviates Neuropathic Pain in Experimental Models of Peripheral Nerve Injury. Pharmaceutics. 2021 Jun 24;13(7):947.
[2]. Baranowska B, et al. Direct effect of cortistatin on GH release from cultured pituitary cells in the rat. Neuro Endocrinol Lett. 2006 Feb-Apr;27(1-2):153-6. [3]. Spier AD, et al. Cortistatin: a member of the somatostatin neuropeptide family with distinct physiological functions. Brain Res Brain Res Rev. 2000 Sep;33(2-3):228-41. [4]. Benitez R, et al. Cortistatin regulates fibrosis and myofibroblast activation in experimental hepatotoxic- and cholestatic-induced liver injury. Br J Pharmacol. 2022 May;179(10):2275-2296. |
| Additional Infomation |
Cortistatin 29 (rat/mouse sequence: dRNMPCKNFFWKTFSSCK) is a neuropeptide that shares structural homology with somatostatin but has distinct pharmacological properties, including high affinity for all SSTR subtypes. It is expressed predominantly in the brain cortex and hippocampus and has been implicated in sleep regulation, memory, and pain modulation. It is not approved for clinical use.
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| Molecular Formula |
C161H242N46O41S2
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|---|---|
| Molecular Weight |
3539.77
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| Appearance |
Typically exists as solid at room temperature
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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) |
H2O :~100 mg/mL (~28.25 mM)
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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 | 0.2825 mL | 1.4125 mL | 2.8250 mL | |
| 5 mM | 0.0565 mL | 0.2825 mL | 0.5650 mL | |
| 10 mM | 0.0283 mL | 0.1413 mL | 0.2825 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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