Physicochemical Properties
| Molecular Formula | C161H242N46O41S2 |
| Molecular Weight | 3539.77 |
| Appearance | Typically exists as solid at room temperature |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| 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) |
| 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]. |
| 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. |
| 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. |
Solubility Data
| Solubility (In Vitro) | H2O :~100 mg/mL (~28.25 mM) |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (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 |