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| 1mg |
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| Other Sizes |
| Targets |
SDP116 targets the adhesion G protein-coupled receptor GPR116 (ADGRF5), a member of the adhesion GPCR family. It acts as a synthetic agonist that binds to and activates the GPR116 receptor, thereby modulating downstream signaling pathways. Activation of GPR116 by this Stachel-derived peptide has been shown to inhibit the activation of muscle stem cells (MuSCs), highlighting its role in regulating cellular differentiation and quiescence.
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| ln Vitro |
SDP116, a peptide produced from stachel, suppresses MuSC activation while stimulating GPR116 [1].
SDP116 has ADGRF5 agonist activity, demonstrating efficacy in stimulating the GPR116 receptor. The primary in vitro activity is the modulation of muscle stem cell (MuSC) behavior, where stimulation of GPR116 by SDP116 leads to the inhibition of MuSC activation. This effect makes it a valuable tool for dissecting the signaling pathways downstream of GPR116 in cellular models. |
| ln Vivo |
In vivo activity data for SDP116 have not been detailed in the provided references. However, based on its mechanism as a GPR116 agonist, it is hypothesized to influence processes involving muscle regeneration and stem cell quiescence. Further in vivo validation is required to confirm its effects on muscle physiology and potential therapeutic applications for muscular disorders.
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| Enzyme Assay |
SDP116 is a Stachel-derived peptide agonist of GPR116. A cell-free binding assay for GPCRs can be performed using surface plasmon resonance (SPR) to directly measure the interaction between SDP116 and purified GPR116 protein. Alternatively, a radioligand competition binding assay using membranes from cells overexpressing GPR116 can be employed to determine the binding affinity (Kd) and kinetic parameters of SDP116.
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| Cell Assay |
For cell-based functional assays, cells expressing recombinant GPR116 are used to assess agonist activity. Common readouts include measuring downstream signaling events such as cAMP accumulation (using HTRF or ELISA), intracellular calcium release (using Fluo-4 dye and a plate reader), or recruitment of beta-arrestin. Cells are treated with varying concentrations of SDP116 to generate a concentration-response curve and determine its potency (EC50).
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| Animal Protocol |
A standard protocol for studying the effect of SDP116 in vivo involves rodent models of muscle injury and regeneration. Muscle stem cell activation is induced via cardiotoxin (CTX) injection into the tibialis anterior (TA) muscle of mice. Following injury, SDP116 is administered locally (intramuscular) or systemically. The effect on MuSC activation is then evaluated by immunofluorescence staining for MuSC markers (e.g., Pax7) and proliferation markers (e.g., Ki67) in muscle sections.
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| ADME/Pharmacokinetics |
The pharmacokinetic profile of SDP116 is not detailed in the provided references. As a synthetic peptide, its in vivo stability and half-life are expected to be short due to rapid proteolytic degradation. The powder should be stored at -20degC for up to 3 years, protected from moisture and light. For in vivo studies, it would require formulation in a vehicle such as PBS or a DMSO/PEG solution.
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| Toxicity/Toxicokinetics |
No specific toxicity data are available for SDP116. As a research-grade peptide agonist, it is used at relatively low concentrations in vitro and in vivo. The primary safety consideration is the potential for off-target effects due to the broad expression of adhesion GPCRs, but no detailed toxicity studies have been published. Standard laboratory safety precautions should be followed.
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| References |
[1]. Lilian M Demberg, et al. Activation of Adhesion G Protein-coupled Receptors: AGONIST SPECIFICITY OF STACHEL SEQUENCE-DERIVED PEPTIDES. J Biol Chem. 2017 Mar 17;292(11):4383-4394.
[2]. Charlotte Sénéchal, et al. The adhesion G-protein-coupled receptor Gpr116 is essential to maintain the skeletal muscle stem cell pool. Cell Rep. 2022 Nov 15;41(7):111645. |
| Additional Infomation |
SDP116 is a research-grade peptide and is not approved for clinical use. It is a synthetic Stachel-derived agonist of the adhesion GPCR GPR116 and is used as a tool to study stem cell biology, particularly the regulation of muscle stem cell activation. This product is for research use only and not for human therapeutic applications. Store at -20degC in a sealed container to maintain stability.
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| Molecular Formula |
C60H93N13O23S
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| Appearance |
White to off-white solid powder
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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 :~1.11 mg/mL (~0.79 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.) |
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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