Art. -Nr.: HY-182539

DD04107

Kundenbewertung

Based on 1 Customer Validation

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

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1202877-06-2
Formel: C₄₈H₈₈N₁₄O₁₂S
Molecular Weight:1085.36

Speicherung:

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)

Kundenspezifische Peptidsynthese

DD04107 Chemical Structure

CAS. Nr.: 1202877-06-2

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

CAS. Nr. 1202877-06-2
Appearance Solid
Molecular Weight 1085.36
Formel C₄₈H₈₈N₁₄O₁₂S
Sequence

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

palmitoyl-EEMQRR-NH2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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)

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : ≥ 100 mg/mL (92.14 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9214 mL

4.6068 mL

9.2135 mL

5 mM

0.1843 mL

0.9214 mL

1.8427 mL

10 mM

0.0921 mL

0.4607 mL

0.9214 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

DD04107

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DD04107 Related Classifications

HY-182539 Related Classifications