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| Targets |
GDC-0310 targets Nav1.7, a voltage-gated sodium channel that is predominantly expressed in peripheral sensory neurons and plays a critical role in pain signaling. Nav1.7 is a validated target for pain management, and mutations in the gene encoding Nav1.7 are associated with pain disorders. By inhibiting hNav1.7 with an IC50 of 0.6 nM, GDC-0310 blocks sodium ion influx in sensory neurons, thereby reducing pain signal transmission. GDC-0310 also targets CCR2.
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| ln Vitro |
GDC-0310's in vivo EC50 is 1.1 μM, while Nav1.7's Ki is 1.8 nM[1].
In vitro, GDC-0310 is a selective Nav1.7 inhibitor with an IC50 of 0.6 nM for hNav1.7. It is an acyl-sulfonamide inhibitor that shows high potency and selectivity for Nav1.7 over other sodium channel isoforms. The compound's potent inhibition of Nav1.7 makes it a valuable tool for studying pain signaling and for developing pain therapeutics. It also targets CCR2, supporting research into immune cell trafficking. |
| ln Vivo |
GDC-0310 displays dramatically increased Nav selectivity and ADME characteristics [1]. The t1/2 values of GDC-0310 in rats (5 mg/kg, i.v.), dogs (1 mg/kg, i.v.), and cynomolgus monkeys (2 mg/kg, i.v.) were 5 hours and 46, respectively. hours and 4.4 hours[1].
In vivo, GDC-0310 is an oral primary clinical candidate for the study of pain. By inhibiting Nav1.7, the compound may reduce pain signal transmission and have therapeutic potential for various pain conditions. The compound's oral bioavailability and in vivo efficacy support its development as a pain therapeutic. However, specific in vivo efficacy data have not been detailed in the available literature. |
| Enzyme Assay |
For in vitro electrophysiology assays, cells expressing hNav1.7 channels are used in patch-clamp recordings. GDC-0310 is added at various concentrations (0.001-100 nM), and sodium currents are measured. IC50 values are calculated by fitting dose-response curves of current inhibition versus compound concentration. Selectivity is assessed by testing the compound against other sodium channel isoforms.
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| Cell Assay |
For cell-based assays, cells expressing Nav1.7 channels are treated with GDC-0310 at concentrations ranging from 0.001-1000 nM. Sodium channel activity is assessed by measuring sodium influx using fluorescent dyes or by electrophysiological recordings. For CCR2-related studies, chemotaxis assays can be performed to assess the compound's effects on immune cell migration.
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| Animal Protocol |
For in vivo efficacy studies, animal models of pain (such as formalin test, CFA-induced inflammatory pain, or neuropathic pain models) would be used. GDC-0310 would be administered orally at doses determined from pharmacokinetic studies. Pain behaviors would be assessed, and analgesic efficacy would be measured. However, specific in vivo protocols for GDC-0310 have not been detailed in the available literature.
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| ADME/Pharmacokinetics |
GDC-0310 is orally available. It is soluble in DMSO. Storage is recommended at -20°C for long-term stability. Further detailed PK parameters including half-life, Cmax, AUC, and tissue distribution would be available from the primary literature. The compound is for research use only and is not intended for human or veterinary use.
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| Toxicity/Toxicokinetics |
Toxicological data for GDC-0310 would be available from preclinical studies. As a clinical candidate, it has undergone safety evaluation. Common adverse effects associated with Nav1.7 inhibitors may include off-target effects on other sodium channels. As a research compound, standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
GDC-0310 is a selective, orally available Nav1.7 inhibitor with an IC50 of 0.6 nM for hNav1.7. It is an oral primary clinical candidate for the study of pain. GDC-0310 also targets CCR2. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C25H29CL2FN2O4S
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|---|---|
| Molecular Weight |
543.478167295456
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| Exact Mass |
542.12
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| CAS # |
1788063-52-4
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| PubChem CID |
118110531
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| Appearance |
White to off-white solid powder
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| LogP |
5.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
822
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1C=C(C=C(C=1)[C@H](C)N1CCC(COC2=CC(=C(C(NS(C)(=O)=O)=O)C=C2C2CC2)F)CC1)Cl
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| InChi Key |
SXOAHIZWCZOILH-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C25H29Cl2FN2O4S/c1-15(18-9-19(26)11-20(27)10-18)30-7-5-16(6-8-30)14-34-24-13-23(28)22(12-21(24)17-3-4-17)25(31)29-35(2,32)33/h9-13,15-17H,3-8,14H2,1-2H3,(H,29,31)/t15-/m0/s1
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| Chemical Name |
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)ethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamide
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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 |
| 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) |
DMSO : ~4 mg/mL (~7.36 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 | 1.8400 mL | 9.2000 mL | 18.3999 mL | |
| 5 mM | 0.3680 mL | 1.8400 mL | 3.6800 mL | |
| 10 mM | 0.1840 mL | 0.9200 mL | 1.8400 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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