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DD04107

DD04107 is a neuronal exocytosis inhibitor with a rat Syt1-C2B domain binding K_a 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.

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No. CAS: 1202877-06-2
Fòrmula: C₄₈H₈₈N₁₄O₁₂S
Peso molecular:1085.36

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

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DD04107 Chemical Structure

No. CAS: 1202877-06-2

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Actividad biológica
- Descripciòn
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
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Actividad biológica

Descripciòn

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 K_D 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.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t	V_ss	MRT_0-t	T_max
Rat^[1]	0.5 mg/kg	i.v.	46.6 mg/L	78.3 mg·h/L	0.013 L	3.87 h	0 h
Rat^[1]	5 mg/kg	i.v.	461 mg/L	184 mg·h/L	0.020 L	2.71 h	0 h
Rat^[1]	10 mg/kg	s.c.	19.7 mg/L	283 mg·h/L	0.112 L	12.7 h	10.5 h

In Vivo

DD04107 (5 mg/kg; i.m.; single dose) displays potent in vivo anti-inflammatory and antihyperalgesic activity against carrageenan-induced inflammatory pain in Wistar rats^[1].
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.

Animal Model:

Wistar (male, ~150 g, intraplantar injection of 2% carrageenan solution)^[1]
Dosage:

5 mg/kg
Administration:

i.m.; single dose
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.

Animal Model:

Wistar (male, ~200 g, intraplantar injection of 1:1 oil/saline CFA emulsion)^[1]
Dosage:

1 mg/kg
Administration:

i.m.; single dose
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.

Animal Model:

Sprague-Dawley (male, ~300 g, intraperitoneal injection of vincristine sulfate three times per week for 2 weeks)^[1]
Dosage:

0.1-0.5 mg/kg
Administration:

s.c.; single dose
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.

Animal Model:

Sprague-Dawley (male, ~250 g, intraperitoneal injection of paclitaxel on days 1, 3, 5, 7)^[1]
Dosage:

0.5 mg/kg
Administration:

s.c.; single dose
Result:

Significantly attenuated paclitaxel-induced mechanical allodynia.
Antiallodynic effect lasted up to 12 days post-administration.

Animal Model:

CD1 (male, 30-40 g, intraperitoneal injection of streptozotocin, blood glucose >250 mg/dl)^[1]
Dosage:

0.5-5 mg/kg
Administration:

s.c.; single dose
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.

Animal Model:

C3H/He (male, 20-25 g, intratibial injection of 10⁵ NCTC 2472 osteosarcoma cells)^[1]
Dosage:

0.1-3.0 mg/kg
Administration:

s.c.; single dose
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.

Animal Model:

Sprague-Dawley (male, ~300 g)^[1]
Dosage:

5 mg/kg
Administration:

s.c.; single dose
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

No. CAS 1202877-06-2
Peso molecular 1085.36
Fòrmula C₄₈H₈₈N₁₄O₁₂S
Sequence

palmitoyl-Glu-Glu-Met-Gln-Arg-Arg-NH2
Sequence Shortening

palmitoyl-EEMQRR-NH2
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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]

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100 mg

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