2. GPCR/G Protein Neuronal Signaling
  3. CGRP Receptor
  4. DD04107

DD04107 (palmitoyl-EEMQRR-NH2) 是一种神经元胞吐抑制剂，其与大鼠 Syt1-C2B 结构域的结合 Ka 值为 2.4 μM。DD04107 干扰 synaptobrevin-syntaxin-SNAP-25 复合物的形成以及 Syt1-SNARE 复合物的相互作用，从而阻断 α-降钙素基因相关肽 (α-CGRP) 从初级感觉神经元的胞吐释放。DD04107 阻断炎症离子通道向伤害感受器质膜的募集。DD04107 在慢性疼痛模型中表现出抗痛觉过敏、抗异常性疼痛和体内镇痛活性。DD04107 具有双室药代动力学全身分布特征，且无运动功能障碍相关的副作用。 DD04107 可用于慢性炎症性疼痛、神经性疼痛、骨肉瘤疼痛、化疗引起的周围神经病变、糖尿病神经病变、炎症性疼痛的研究。

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Custom Peptide Synthesis

DD04107

DD04107 Chemical Structure

CAS No. : 1202877-06-2

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DD04107 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DD04107 (palmitoyl-EEMQRR-NH2) is a neuronal exocytosis inhibitor with a rat Syt1-C2B domain binding Ka 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 induces antihyperalgesia, antiallodynia, and in vivo analgesic activity in chronic pain models. DD04107 exhibits bicompartmental pharmacokinetic systemic distribution and lacks locomotor impairment-related side effects. DD04107 can be used for the research of chronic inflammatory pain, neuropathic pain, osteosarcoma pain, chemotherapy-induced peripheral neuropathy, diabetic neuropathy, inflammatory pain[1][2].

体外研究
(In Vitro)

DD04107 (5-50 μM；1 小时预处理) 可剂量依赖性地抑制辣椒素诱导的体外培养新生 Wistar 大鼠背根节初级感觉神经元释放 α-CGRP，在 5 μM 浓度下即可观察到显著抑制作用，50 μM 浓度下的抑制作用更强[1]。
DD04107 (10 μM) 对大多数受试神经元受体未表现出显著结合亲和力，仅在一小部分受体中观察到弱相互作用 (IC50 >10 μM)[1]。
DD04107 (0.5-5 μM) 在表达 hERG 通道的人胚肾 293 细胞中，0.5 μM 和 5 μM 浓度下均不会抑制 hERG 通道活性[1]。
DD04107 (10 μM；1 小时) 可使新生 Wistar 大鼠背根神经节分离得到的初级伤害性感觉神经元中辣椒素诱导的 α-CGRP 胞吐作用抑制 47%[2]。
DD04107 可选择性结合大鼠 Syt1-C2B 结构域，其 KD 值为 2.4 μM，且不与大鼠 Syt7-C2B 结构域发生相互作用[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DD04107 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-t Vss MRT0-t Tmax
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
体内研究
(In Vivo)

DD04107 (5 mg/kg；肌肉注射；单次给药) 对 Wistar 大鼠角叉菜胶诱导的炎性疼痛表现出强效的体内抗炎及抗痛觉过敏活性[1]。
DD04107 (1 mg/kg；肌内注射；单次给药) 在 Wistar 大鼠中对 CFA 诱导的慢性炎性疼痛表现出持久 (≥5 天) 的抗痛觉过敏和抗异常性疼痛活性[1]。
DD04107 (0.1-0.5 mg/kg；皮下注射；单次给药) 对 Sprague-Dawley 大鼠中长春新碱诱导的神经性疼痛具有持久 (长达 10 天) 的剂量依赖性抗痛觉过敏活性[1]。
DD04107 (0.5 mg/kg；皮下注射；单次给药) 可在 Sprague-Dawley 大鼠中对紫杉醇诱导的神经病理性疼痛产生长效 (长达 12 天) 的抗异常痛觉活性[1]。
DD04107 (0.5-5 mg/kg；皮下注射；单次给药) 对 CD1 小鼠链脲佐菌素诱导的糖尿病神经病理性疼痛表现出剂量依赖性的抗异常痛觉活性，持续时间可达 24 小时[1]。
DD04107 (0.1-3.0 mg/kg；皮下注射；单次给药) 在 C3H/He 小鼠中对骨肉瘤诱导的骨癌疼痛表现出强效、持久 (可达 7-8 天) 的剂量依赖性抗痛觉过敏和抗异常痛觉活性[1]。
DD04107 (5 mg/kg；皮下注射；单次给药) 在健康 Sprague-Dawley 大鼠中产生不依赖阿片受体介导的镇痛活性[1]。

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.
分子量

1085.36

Formula

C48H88N14O12S
CAS 号
Sequence

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

palmitoyl-EEMQRR-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DD04107 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DD041071202877-06-2DD 04107DD-04107CGRP ReceptorCalcitonin gene-related peptide receptornociceptor plasma membranescalcitonin gene-related peptidehuman embryonic kidney 293 cellssynaptobrevin-syntaxin-SNAP-25 complexCa2+-dependent neuronal exocytosisα-calcitonin gene-related peptideSNARE complexprimary sensory neuronsrat Syt1-C2B domainSynaptotagmin-1 (Syt1)-C2B domainInhibitorinhibitorinhibit

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