Calcitonin Gene Related Peptide (CGRP) II, rat TFA, an activator of CGRP receptors, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide (CGRP) II, rat TFA may be utilized in cardiovascular disease study.

Physicochemical Properties

Molecular Formula	C165H268F3N51O52S2
Molecular Weight	3919.33
Related CAS #	Calcitonin Gene Related Peptide (CGRP) II, rat;99889-63-1
Appearance	Solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	With an EC50 value of 0.56 nM, rat TFA containing calcitonin gene related protein (CGRP) II causes vasodilator effects in small-diameter pig left anterior descending (LAD) coronary arteries[1]. Rat TFA, calcitonin Gene Related Peptide (CGRP) II, has an EC50 value of 83 μM and relaxes the spontaneous tone in isolated internal anal sphincter (IAS) strips[2]. Calcitonin Gene Related Peptide (CGRP) II, rat TFA (rβCGRP), in cells co-expressing mRAMP1 (mouse receptor-activity-modifying protein 1) and rCRLR (rat calcitonin receptor-like receptor), reduces [125I]hαCGRP binding (IC50: 7 nM) and promotes cAMP buildup (EC50: 0.56 nM)[3]. With an approximate IC50 value of 2.8 nM, calcitonin gene related protein II, rat TFA (rat-βCGRP, 0.01-100 nM) causes endothelium-independent relaxations in the coronary arteries of both male and female Sprague-Dawley rats[4].
ln Vivo	In male Sprague-Dawley rats, a bolus injection of 0.3 μg/kg of rat-βCGRP (calcitonin gene-related peptide) at 10-minute intervals causes vasodilatation and hypotension[5].
Animal Protocol	Animal/Disease Models: Male SD (Sprague-Dawley) rats[5] Doses: 0.01 ng/kg-3 μg/kg (100 μL), succeeded by a 150 μL isotonic saline flush, at 10 min intervals. Route of Administration: A bolus injection Experimental Results: Induced PA (pial artery) dilatation and increased in LCBFFlux (local cortical cerebral blood flow).
References	[1]. Development and potential of non-peptide antagonists for calcitonin-gene-related peptide (CGRP) receptors: evidence for CGRP receptor heterogeneity. Biochem Soc Trans. 2002 Aug;30(4):468-73. [2]. CGRP(2) receptor in the internal anal sphincter of the rat: implications for CGRP receptor classification. Br J Pharmacol. 2000 May;130(2):464-70. [3]. Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function. Mol Cell Endocrinol. 2000 Apr 25;162(1-2):35-43. [4]. Characterization of calcitonin gene-related peptide (CGRP) receptors in intramural coronary arteries from male and female Sprague Dawley rats. Br J Pharmacol. 1998 Apr;123(7):1464-70. [5]. Inhibitory effect of BIBN4096BS on cephalic vasodilatation induced by CGRP or transcranial electrical stimulation in the rat. Br J Pharmacol. 2004 Nov;143(6):697-704.

Solubility Data

Solubility (In Vitro)

H2O :~25 mg/mL (~6.38 mM)

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.2551 mL	1.2757 mL	2.5515 mL
	5 mM	0.0510 mL	0.2551 mL	0.5103 mL
	10 mM	0.0255 mL	0.1276 mL	0.2551 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.