5'-IodoresiniferatoxinPotent, silent TRPV1 antagonist CAS# 535974-91-5 |
- Verteporfin
Catalog No.:BCC3690
CAS No.:129497-78-5
- Miglustat hydrochloride
Catalog No.:BCC5186
CAS No.:210110-90-0
- Hydrochlorothiazide
Catalog No.:BCC4786
CAS No.:58-93-5
- Miglustat
Catalog No.:BCC5187
CAS No.:72599-27-0
- TPT-260
Catalog No.:BCC5171
CAS No.:769856-81-7
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 535974-91-5 | SDF | Download SDF |
PubChem ID | 16219535 | Appearance | Powder |
Formula | C37H39IO9 | M.Wt | 754.6 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | Iodoresiniferatoxin, 5'-IRTX | ||
Solubility | Soluble in DMSO and to 100 mM in ethanol | ||
Chemical Name | [(1R,2R,6R,10S,11R,15R,17R)-13-benzyl-6-hydroxy-4,17-dimethyl-5-oxo-15-prop-1-en-2-yl-12,14,18-trioxapentacyclo[11.4.1.01,10.02,6.011,15]octadeca-3,8-dien-8-yl]methyl 2-(4-hydroxy-3-iodo-5-methoxyphenyl)acetate | ||
SMILES | CC1CC2(C3C4C1(C5C=C(C(=O)C5(CC(=C4)COC(=O)CC6=CC(=C(C(=C6)I)O)OC)O)C)OC(O3)(O2)CC7=CC=CC=C7)C(=C)C | ||
Standard InChIKey | TZUJORCXGLGWDV-RYACRXIZSA-N | ||
Standard InChI | InChI=1S/C37H39IO9/c1-20(2)35-16-22(4)37-26(33(35)45-36(46-35,47-37)18-23-9-7-6-8-10-23)12-25(17-34(42)29(37)11-21(3)32(34)41)19-44-30(39)15-24-13-27(38)31(40)28(14-24)43-5/h6-14,22,26,29,33,40,42H,1,15-19H2,2-5H3/t22-,26+,29-,33-,34-,35-,36?,37-/m1/s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Potent and silent vanilloid receptor antagonist, 40-fold more potent than capsazepine. Binds to TRPV1 (VR1) receptors expressed in HEK293 cells with a Ki of 5.8 nM. |
5'-Iodoresiniferatoxin Dilution Calculator
5'-Iodoresiniferatoxin Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.3252 mL | 6.626 mL | 13.2521 mL | 26.5041 mL | 33.1301 mL |
5 mM | 0.265 mL | 1.3252 mL | 2.6504 mL | 5.3008 mL | 6.626 mL |
10 mM | 0.1325 mL | 0.6626 mL | 1.3252 mL | 2.6504 mL | 3.313 mL |
50 mM | 0.0265 mL | 0.1325 mL | 0.265 mL | 0.5301 mL | 0.6626 mL |
100 mM | 0.0133 mL | 0.0663 mL | 0.1325 mL | 0.265 mL | 0.3313 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- Secolongifolenediol
Catalog No.:BCN6989
CAS No.:53587-37-4
- H-Tyr-OBzl.TosOH
Catalog No.:BCC3124
CAS No.:53587-11-4
- 5-Galloylquinic acid
Catalog No.:BCN3060
CAS No.:53584-43-3
- Beta-Amyrenonol acetate
Catalog No.:BCN4620
CAS No.:5356-56-9
- (-)-Bicuculline methochloride
Catalog No.:BCN3763
CAS No.:53552-05-9
- Diaveridine
Catalog No.:BCC8936
CAS No.:5355-16-8
- Benzoyl-L-histidine
Catalog No.:BCC8866
CAS No.:5354-94-9
- Apigenin 7-O-methylglucuronide
Catalog No.:BCN5708
CAS No.:53538-13-9
- Luteolin-3-O-beta-D-glucuronide
Catalog No.:BCN3826
CAS No.:53527-42-7
- Durantoside I
Catalog No.:BCN4621
CAS No.:53526-67-3
- Durantoside II
Catalog No.:BCN4622
CAS No.:53526-66-2
- 7-Amino-4-(Trifluoromethyl)Coumarin
Catalog No.:BCC9208
CAS No.:53518-15-3
- Ethionamide
Catalog No.:BCC3778
CAS No.:536-33-4
- Perillyl alcohol
Catalog No.:BCN3876
CAS No.:536-59-4
- 1-Hydroxyrutaecarpine
Catalog No.:BCN5709
CAS No.:53600-24-1
- GMQ hydrochloride
Catalog No.:BCC6351
CAS No.:5361-15-9
- Teucvin
Catalog No.:BCN8375
CAS No.:53625-15-3
- Vindesine
Catalog No.:BCN2607
CAS No.:53643-48-4
- Dehydrobruceantin
Catalog No.:BCN7617
CAS No.:53662-98-9
- 4,6-Dimethoxy-2H-1-benzopyran-2-one
Catalog No.:BCN3452
CAS No.:53666-78-7
- O-1918
Catalog No.:BCC7313
CAS No.:536697-79-7
- ICI 89406
Catalog No.:BCC6807
CAS No.:53671-71-9
- QX 222
Catalog No.:BCC6906
CAS No.:5369-00-6
- QX 314 chloride
Catalog No.:BCC7326
CAS No.:5369-03-9
Genotype-dependent responsivity to inflammatory pain: A role for TRPV1 in the periaqueductal grey.[Pubmed:27520401]
Pharmacol Res. 2016 Nov;113(Pt A):44-54.
Negative affective state has a significant impact on pain, and genetic background is an important moderating influence on this interaction. The Wistar-Kyoto (WKY) inbred rat strain exhibits a stress-hyperresponsive, anxiety/depressive-like phenotype and also displays a hyperalgesic response to noxious stimuli. Transient receptor potential subfamily V member 1 (TRPV1) within the midbrain periaqueductal grey (PAG) plays a key role in regulating both aversive and nociceptive behaviour. In the present study, we investigated the role of TRPV1 in the sub-columns of the PAG in formalin-evoked nociceptive behaviour in WKY versus Sprague-Dawley (SD) rats. TRPV1 mRNA expression was significantly lower in the dorsolateral (DL) PAG and higher in the lateral (L) PAG of WKY rats, compared with SD counterparts. There were no significant differences in TRPV1 mRNA expression in the ventrolateral (VL) PAG between the two strains. TRPV1 mRNA expression significantly decreased in the DLPAG and increased in the VLPAG of SD, but not WKY rats upon intra-plantar formalin administration. Intra-DLPAG administration of either the TRPV1 agonist capsaicin, or the TRPV1 antagonist 5'-Iodoresiniferatoxin (5'-IRTX), significantly increased formalin-evoked nociceptive behaviour in SD rats, but not in WKY rats. The effects of capsaicin were likely due to TRPV1 desensitisation, given their similarity to the effects of 5'-IRTX. Intra-VLPAG administration of capsaicin or 5'-IRTX reduced nociceptive behaviour in a moderate and transient manner in SD rats, and similar effects were seen with 5'-IRTX in WKY rats. Intra-LPAG administration of 5'-IRTX reduced nociceptive behaviour in a moderate and transient manner in SD rats, but not in WKY rats. These results indicate that modulation of inflammatory pain by TRPV1 in the PAG occurs in a sub-column-specific manner. The data also provide evidence for differences in the expression of TRPV1, and differences in the effects of pharmacological modulation of TRPV1 in specific PAG sub-columns, between WKY and SD rats, suggesting that TRPV1 expression and/or functionality in the PAG plays a role in hyper-responsivity to noxious stimuli in a genetic background prone to negative affect.
Capsaicin activation of glutamatergic synaptic transmission in the rat locus coeruleus in vitro.[Pubmed:12205187]
J Physiol. 2002 Sep 1;543(Pt 2):531-40.
The vanilloid receptor protein (VR1) is a well-characterised integrator of noxious stimuli in peripheral sensory neurones. There is evidence for the presence of VR1 in the central nervous system, but little information as to its role there. In this study we have examined the actions of agonists for VR1 receptors in the rat locus coeruleus (LC), using whole-cell patch-clamp recordings from acutely isolated neurones and neurones in slices. Superfusion with capsaicin resulted in a concentration-dependent increase in the frequency of isolated miniature excitatory postsynaptic currents (mEPSCs) in LC neurones. The mean amplitude of the mEPSCs was not affected by capsaicin. The effects of capsaicin (1 microM) were abolished by the VR1 receptor antagonists capsazepine (10 microM) and iodoresiniferatoxin (300 nM). Removal of extracellular Ca2+ abolished the capsaicin-induced increase in frequency of mEPSCs. Capsaicin superfusion had no consistent effects on evoked excitatory postsynaptic currents. Capsaicin superfusion also resulted in the release of an adrenoceptor agonist in the LC but did not affect the membrane currents of acutely isolated LC neurones. These data demonstrate that the VR1 receptor appears to be located presynaptically on afferents to the LC, and that activation of VR1 may serve to potentiate the release of glutamate and adrenaline/noradrenaline in this brain region.