| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
GalR2 and GalR3 receptors. Spexin binds to GALR2 with high affinity (Ki ~ 0.5‑5 nM) and to GALR3 with moderate affinity (Ki ~ 10‑50 nM). No significant binding to GALR1 (Ki > 1 microM). It also shows weak activity at the angiotensin AT1 receptor.
|
|---|---|
| ln Vitro |
In vitro, spexin inhibits forskolin‑stimulated cAMP accumulation in CHO cells expressing human GALR2 (IC50 ~ 1‑10 nM). It activates ERK1/2 phosphorylation and induces calcium mobilization in some systems. In hypothalamic neurons, spexin reduces NPY expression and increases POMC expression, suggesting anorexigenic effects.
|
| ln Vivo |
In vivo, spexin (50‑200 microg/kg i.p. or i.c.v.) reduces food intake in mice and rats. It also lowers blood pressure when administered i.v. (10‑100 nmol/kg). In chronic pain models (CFA injection), spexin (30 nmol i.t.) reduces mechanical allodynia and thermal hyperalgesia. These effects are blocked by GALR2 antagonist.
|
| Enzyme Assay |
Use CHO cell membranes expressing human GALR2 (20 microg protein). Incubate with 0.5 nM [¹2⁵I]‑galanin and spexin (0.01 nM‑10 microM) in 50 mM Tris‑HCl pH 7.4 with 5 mM MgCl2, 0.1% BSA for 60 min at RT. Non‑specific: 1 microM unlabeled galanin. Filter through GF/B, wash, count. Ki ~ 0.5‑5 nM.
|
| Cell Assay |
Seed CHO‑GALR2 cells in 96‑well plates (40,000/well) in DMEM/10% FBS for 48 h. Wash, add 0.5 mM IBMX, incubate 10 min. Then add spexin (0.01 nM‑10 microM) plus 1 microM forskolin for 15 min. Lyse and measure cAMP using ELISA or HTRF. Calculate IC50 for inhibition of cAMP accumulation. Also measure ERK phosphorylation by Western blot or AlphaLISA.
|
| Animal Protocol |
Male C57BL/6 mice (20‑25 g) for food intake. Fast overnight. Inject spexin (50, 100, 200 microg/kg i.p.) or vehicle at the start of the light cycle. Return to home cage with pre‑weighed food. Measure food consumption at 1, 2, 4, and 24 h. Cumulative intake is reduced by spexin. For pain: intrathecal injection (5 microL) of spexin (10‑30 nmol) in mice with CFA‑induced hindpaw inflammation; test mechanical allodynia with von Frey filaments at 30‑180 min post‑injection.
|
| ADME/Pharmacokinetics |
Spexin is a peptide; degraded by proteases. t½ in plasma < 15 min. Does not cross BBB. Often administered i.c.v., i.t., or i.p. For i.v. bolus, volume of distribution approximates plasma volume. Rapid renal clearance. No oral bioavailability. Stability can be improved with PEGylation or D‑amino acid substitution in research.
|
| Toxicity/Toxicokinetics |
Low toxicity. No adverse effects at doses up to 500 microg/kg i.p. in mice. No mutagenicity. At high doses (1 mg/kg i.v.), transient hypotension. Chronic administration not studied extensively. Not approved for human use.
|
| References | |
| Additional Infomation |
Endogenous peptide ligand for GALR2/3. Regulates energy balance, pain, and cardiovascular function. Potential therapeutic target for obesity and chronic pain. Not clinically approved. CAS 1370290‑58‑6. Research grade only.
|
| Molecular Formula |
C74H114N20O19S
|
|---|---|
| Molecular Weight |
1619.88457536697
|
| Exact Mass |
1618.828
|
| CAS # |
1370290-58-6
|
| Related CAS # |
Spexin TFA
|
| PubChem CID |
122705996
|
| Appearance |
White to off-white solid powder
|
| LogP |
-3.6
|
| Hydrogen Bond Donor Count |
21
|
| Hydrogen Bond Acceptor Count |
22
|
| Rotatable Bond Count |
50
|
| Heavy Atom Count |
114
|
| Complexity |
3310
|
| Defined Atom Stereocenter Count |
14
|
| SMILES |
S(C)CC[C@@H](C(N[C@H](C(N[C@@H](CC1C=CC(=CC=1)O)C(N[C@H](C(N[C@H](C(NCC(N[C@@H](C)C(N[C@H](C(N)=O)CCC(N)=O)=O)=O)=O)CCCCN)=O)CC(C)C)=O)=O)CC(C)C)=O)NC([C@H](C)NC([C@H](CCC(N)=O)NC([C@@H]1CCCN1C([C@H]([C@@H](C)O)NC([C@H](CC1=CNC2C=CC=CC1=2)NC([C@H](CC(N)=O)N)=O)=O)=O)=O)=O)=O
|
| InChi Key |
ZZDZBDJTNIOJMF-TWMPYRTRSA-N
|
| InChi Code |
InChI=1S/C74H114N20O19S/c1-37(2)30-52(69(108)87-49(16-11-12-27-75)66(105)82-36-60(100)83-39(5)63(102)85-48(62(80)101)22-24-57(77)97)91-71(110)54(32-42-18-20-44(96)21-19-42)92-70(109)53(31-38(3)4)90-68(107)51(26-29-114-8)86-64(103)40(6)84-67(106)50(23-25-58(78)98)88-73(112)56-17-13-28-94(56)74(113)61(41(7)95)93-72(111)55(89-65(104)46(76)34-59(79)99)33-43-35-81-47-15-10-9-14-45(43)47/h9-10,14-15,18-21,35,37-41,46,48-56,61,81,95-96H,11-13,16-17,22-34,36,75-76H2,1-8H3,(H2,77,97)(H2,78,98)(H2,79,99)(H2,80,101)(H,82,105)(H,83,100)(H,84,106)(H,85,102)(H,86,103)(H,87,108)(H,88,112)(H,89,104)(H,90,107)(H,91,110)(H,92,109)(H,93,111)/t39-,40-,41+,46-,48-,49-,50-,51-,52-,53-,54-,55-,56-,61-/m0/s1
|
| Chemical Name |
(2S)-2-[[(2S)-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]acetyl]amino]propanoyl]amino]pentanediamide
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: 25 mg/mL (15.43 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6173 mL | 3.0866 mL | 6.1733 mL | |
| 5 mM | 0.1235 mL | 0.6173 mL | 1.2347 mL | |
| 10 mM | 0.0617 mL | 0.3087 mL | 0.6173 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
