DD04107
Based on 1 Customer Validation
DD04107 is a neuronal exocytosis inhibitor with a rat Syt1-C2B domain binding Kd of 2.4 μM. DD04107 interferes with synaptobrevin-syntaxin-SNAP-25 complex formation and Syt1-SNARE complex interaction to block α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons. DD04107 blocks inflammatory ion channel recruitment to nociceptor plasma membranes. DD04107 can be used for the research of chronic inflammatory pain, neuropathic pain, osteosarcoma pain, chemotherapy-induced peripheral neuropathy, diabetic neuropathy, inflammatory pain.
For research use only. We do not sell to patients.
- Purity : 99.67%
- CAS No.: 1202877-06-2
- Formula: C48H88N14O12S
- Molecular Weight:1085.36
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
DD04107 (5-50 μM; 1 h pretreatment) dose-dependently inhibits capsaicin-induced α-CGRP release from neonatal Wistar rat dorsal root ganglion primary sensory neurons in culture, with significant inhibition observed at 5 μM and stronger inhibition at 50 μM[1].
DD04107 (10 μM) does not exhibit significant binding affinity for most tested neuronal receptors, with only weak interactions (IC50 > 10 μM) observed for a small subset of receptors[1].
DD04107 (0.5-5 μM) does not inhibit hERG channel activity at 0.5 μM and 5 μM in human embryonic kidney 293 cells expressing hERG channels[1].
DD04107 (10 μM; 1 h) inhibits capsaicin-induced α-CGRP exocytosis from primary sensory nociceptor neurons isolated from neonatal Wistar rat dorsal root ganglia by 47%[2].
DD04107 binds selectively to the rat Syt1-C2B domain with a KD of 2.4 μM, and does not interact with the rat Syt7-C2B domain[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
DD04107 (1 mg/kg; i.m.; single dose) exhibits long-lasting (≥5 days) antihyperalgesic and antiallodynic activity against CFA-induced chronic inflammatory pain in Wistar rats[1].
DD04107 (0.1-0.5 mg/kg; s.c.; single dose) delivers long-lasting (up to 10 days) dose-dependent antihyperalgesic activity against vincristine-induced neuropathic pain in Sprague-Dawley rats[1].
DD04107 (0.5 mg/kg; s.c.; single dose) provides long-lasting (up to 12 days) antiallodynic activity against paclitaxel-induced neuropathic pain in Sprague-Dawley rats[1].
DD04107 (0.5-5 mg/kg; s.c.; single dose) exhibits dose-dependent antiallodynic activity lasting up to 24 hours against streptozotocin-induced diabetic neuropathic pain in CD1 mice[1].
DD04107 (0.1-3.0 mg/kg; s.c.; single dose) delivers potent, long-lasting (up to 7-8 days) dose-dependent antihyperalgesic and antiallodynic activity against osteosarcoma-induced bone cancer pain in C3H/He mice[1].
DD04107 (5 mg/kg; s.c.; single dose) produces antinociceptive activity in healthy Sprague-Dawley rats that is not mediated by opioid receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, ~150 g, intraplantar injection of 2% carrageenan solution)[1]
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Dosage:5 mg/kg
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Administration:i.m.; single dose
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Result:Attenuated paw volume increase to a degree identical to 10 mg/kg diclofenac.
Completely reversed carrageenan-induced mechanical hypersensitivity in the ipsilateral paw.
Did not affect the contralateral paw's nociceptive threshold.
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Animal Model:Wistar (male, ~200 g, intraplantar injection of 1:1 oil/saline CFA emulsion)[1]
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Dosage:1 mg/kg
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Administration:i.m.; single dose
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Result:Produced a near-complete reversal of CFA-induced thermal hyperalgesia starting at ~4 hours post-administration.
Significantly increased mechanical nociceptive threshold and reduced withdrawal response frequency to mechanical stimuli.
Antiallodynic activity lasted at least 5 days post-administration.
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Animal Model:Sprague-Dawley (male, ~300 g, intraperitoneal injection of vincristine sulfate three times per week for 2 weeks)[1]
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Dosage:0.1-0.5 mg/kg
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Administration:s.c.; single dose
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Result:Attenuated vincristine-induced mechanical hyperalgesia in a dose-dependent manner.
Significant antinociception observed at doses as low as 0.1 mg/kg.
Activity lasted up to 10 days post-administration.
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Animal Model:Sprague-Dawley (male, ~250 g, intraperitoneal injection of paclitaxel on days 1, 3, 5, 7)[1]
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Dosage:0.5 mg/kg
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Administration:s.c.; single dose
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Result:Significantly attenuated paclitaxel-induced mechanical allodynia.
Antiallodynic effect lasted up to 12 days post-administration.
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Animal Model:CD1 (male, 30-40 g, intraperitoneal injection of streptozotocin, blood glucose >250 mg/dl)[1]
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Dosage:0.5-5 mg/kg
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Administration:s.c.; single dose
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Result:Reduced streptozotocin-induced mechanical allodynia in a dose-dependent manner, with maximum effect at 4 hours post-administration.
5 mg/kg dose maintained significant activity up to 24 hours post-administration.
Residual non-significant activity detectable at 5 days.
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Animal Model:C3H/He (male, 20-25 g, intratibial injection of 105 NCTC 2472 osteosarcoma cells)[1]
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Dosage:0.1-3.0 mg/kg
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Administration:s.c.; single dose
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Result:Attenuated osteosarcoma-induced thermal hyperalgesia in a dose-dependent manner, with complete reversal at 0.3 mg/kg and significant antinociception at 0.1 mg/kg lasting 2-4 days post-administration.
1 mg/kg dose fully reversed mechanical allodynia, with antiallodynic activity starting 24 hours post-administration and lasting up to 7-8 days.
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Animal Model:Sprague-Dawley (male, ~300 g)[1]
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Dosage:5 mg/kg
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Administration:s.c.; single dose
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Result:Increased mechanical nociceptive threshold over 24 hours.
Antinociceptive effect was unaffected by pretreatment with the opioid receptor antagonist naltrexone.
Naltrexone completely abolished the effect of 3 mg/kg morphine.
Chemical Information
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CAS No. 1202877-06-2
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Appearance Solid
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Molecular Weight 1085.36
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Formula C48H88N14O12S
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Color White to off-white
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Sequence
palmitoyl-Glu-Glu-Met-Gln-Arg-Arg-NH2
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Sequence Shortening
palmitoyl-EEMQRR-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
H2O : ≥ 100 mg/mL (92.14 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Two-electrode voltage clamp in Xenopus oocytes
Two-electrode voltage clamp measures whole-oocyte membrane current from Xenopus oocytes expressing exogenous ion channels, receptors, or transporters; one intracellular microelectrode senses membrane voltage, and the second injects current so the amplifier can hold the membrane at command voltages while recording the compensating current as the functional readout. The method is suited to Xenopus oocytes because their large size supports microinjection and intracellular electrode impalement, but the large membrane area can limit voltage-clamp speed and accuracy, especially for large or fast currents.
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
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Primary Dorsal Root Ganglion Sensory Neuron Culture
Primary dorsal root ganglion sensory neuron culture isolates DRG neuronal somata from rodent or human ganglia, dissociates tissue enzymatically and mechanically, and maintains post-mitotic sensory neurons in vitro for readouts such as neurite outgrowth, immunocytochemical marker expression, calcium imaging, electrophysiology, RNA/protein analysis, or neuropeptide release assays. The method reflects peripheral sensory neuron biology because DRG neurons are primary sensory neurons whose cell bodies reside in dorsal root ganglia and whose cultured dissociated cells can retain neuronal morphology, sensory-neuron marker expression, and stimulus-responsive properties depending on the downstream assay.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Ponsati B, et al. An inhibitor of neuronal exocytosis (DD04107) displays long-lasting in vivo activity against chronic inflammatory and neuropathic pain. J Pharmacol Exp Ther. 2012;341(3):634-645. [Content Brief]
[2]. Butrón D, et al. DD04107-Derived neuronal exocytosis inhibitor peptides: Evidences for synaptotagmin-1 as a putative target. Bioorg Chem. 2021;115:105231. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.9214 mL | 4.6068 mL | 9.2135 mL | 23.0338 mL |
| 5 mM | 0.1843 mL | 0.9214 mL | 1.8427 mL | 4.6068 mL | |
| 10 mM | 0.0921 mL | 0.4607 mL | 0.9214 mL | 2.3034 mL | |
| 15 mM | 0.0614 mL | 0.3071 mL | 0.6142 mL | 1.5356 mL | |
| 20 mM | 0.0461 mL | 0.2303 mL | 0.4607 mL | 1.1517 mL | |
| 25 mM | 0.0369 mL | 0.1843 mL | 0.3685 mL | 0.9214 mL | |
| 30 mM | 0.0307 mL | 0.1536 mL | 0.3071 mL | 0.7678 mL | |
| 40 mM | 0.0230 mL | 0.1152 mL | 0.2303 mL | 0.5758 mL | |
| 50 mM | 0.0184 mL | 0.0921 mL | 0.1843 mL | 0.4607 mL | |
| 60 mM | 0.0154 mL | 0.0768 mL | 0.1536 mL | 0.3839 mL | |
| 80 mM | 0.0115 mL | 0.0576 mL | 0.1152 mL | 0.2879 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
DD04107 Related Classifications
HY-182539 Related Classifications
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Keywords
- DD04107
- 1202877-06-2
- DD 04107
- DD-04107
- CGRP Receptor
- nociceptor plasma membranes
- calcitonin gene-related peptide
- human embryonic kidney 293 cells
- synaptobrevin-syntaxin-SNAP-25 complex
- Ca2+-dependent neuronal exocytosis
- α-calcitonin gene-related peptide
- SNARE complex
- primary sensory neurons
- rat Syt1-C2B domain
- Synaptotagmin-1 (Syt1)-C2B domain
- Inhibitor
- inhibitor
- inhibit